Ruxolitinib sulfate(Synonyms: INCB018424 sulfate)

发表于2024年11月2日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Ruxolitinib sulfate (Synonyms: INCB018424 sulfate)

Ruxolitinib sulfate (INCB018424 sulfate) 是一种有效的 JAK1/2 抑制剂，IC₅₀ 值为 3.3 nM/2.8 nM，选择性是对 JAK3 的 130 倍。

Ruxolitinib sulfate Chemical Structure

CAS No. : 1092939-16-6

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Ruxolitinib sulfate 的其他形式现货产品:

Ruxolitinib Ruxolitinib (S enantiomer) Ruxolitinib phosphate

生物活性

Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC₅₀s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.

IC₅₀ & Target^[1]

JAK2

2.8 nM (IC₅₀)

JAK1

3.3 nM (IC₅₀)

Tyk2

19 nM (IC₅₀)

JAK3

428 nM (IC₅₀)

体外研究
(In Vitro)

Ruxolitinib sulfate (INCB018424 sulfate) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation, markedly increases apoptosis in a dose dependent manner, and at 64 nM results in a doubling of cells with depolarized mitochondria in Ba/F3 cells. Ruxolitinib demonstrates remarkable potency against erythroid colony formation with IC₅₀ of 67 nM, and inhibits proliferating of erythroid progenitors from normal donors and polycythemia vera patients with IC₅₀ values of 407 nM and 223 nM, respectively^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ruxolitinib (INCB018424 sulfate; 180 mg/kg, orally, twice a day) results in survive rate of greater than 90% by day 22 and markedly reduces splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminated neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects in a JAK2V617F-driven mouse model^[1].
In the Ruxolitinib group, the primary end point is reached in 41.9% of patients, as compared with 0.7% in the placebo group in the double-blind trial of myelofibrosis. Ruxolitinib results in maintaining of reduction in spleen volume and improvement of 50% or more in the total symptom score^[2].
Ruxolitinib (15 mg twice daily) treatment leads a total of 28% of the patients to have at least a 35% reduction in spleen volume at week 48 in patients with myelofibrosis, as compared with 0% in the group receiving the best available therapy. The mean palpable spleen length has decreased by 56% with Ruxolitinib but has increased by 4% with the best available therapy at week 48. Patients in the ruxolitinib group has an improvement in overall quality-of-life measures and a reduction in symptoms associated with myelofibrosis^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

404.44

Formula

C₁₇H₂₀N₆O₄S

CAS 号

1092939-16-6

中文名称

鲁索利替尼硫酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117.

[2]. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807.

[3]. Harrison C, et al. JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis. N Engl J Med. 2012 Mar 1;366(9):787-98.

Kinase Assay ^[1]	Recombinant proteins are expressed using Sf21 cells and baculovirus vectors and purified with affinity chromatography. JAK kinase assays use a homogeneous time-resolved fluorescence assay with the peptide substrate (-EQEDEPEGDYFEWLE). Each enzyme reaction is carried out with Ruxolitinib or control, JAK enzyme, 500 nM peptide, adenosine triphosphate (ATP; 1mM), and 2% dimethyl sulfoxide (DMSO) for 1 hour. The 50% inhibitory concentration (IC₅₀) is calculated as Ruxolitinib concentration required for inhibition of 50% of the fluorescent signal^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are seeded at 2 × 10³/well of white bottom 96-well plates, treated with Ruxolitinib from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37°C with 5% CO₂. Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values are transformed to percent inhibition relative to vehicle control, and IC₅₀ curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Mice are fed standard rodent chow and provided with water ad libitum. Ba/F3-JAK2V617F cells (10⁵ per mouse) are inoculated intravenously into 6- to 8-week-old female BALB/c mice. Survival is monitored daily, and moribund mice are humanely killed and considered deceased at time of death. Treatment with vehicle (5% dimethyl acetamide, 0.5% methocellulose) or Ruxolitinib begin within 24 hours of cell inoculation, twice daily by oral gavage. Hematologic parameters are measured using a Bayer Advia120 analyzed, and statistical significance is determined using Dunnett testing^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117. [2]. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807. [3]. Harrison C, et al. JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis. N Engl J Med. 2012 Mar 1;366(9):787-98.

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Parsaclisib hydrochloride(Synonyms: INCB050465 hydrochloride)

发表于2024年10月29日由上海金畔生物科技有限公司

Parsaclisib hydrochloride (Synonyms: INCB050465 hydrochloride) 纯度: 98.74%

Parsaclisib hydrochloride (INCB050465 hydrochloride) 是一种有效，选择性和具有口服活性的 PI3Kδ 抑制剂，IC₅₀ 值为 1 nM。Parsaclisib hydrochloride 相对于其他 PI3K I 类同工型的选择性约为 20000 倍。Parsaclisib hydrochloride 可用于研究复发或难治性 B 细胞恶性肿瘤。

Parsaclisib hydrochloride Chemical Structure

CAS No. : 1995889-48-9

规格	价格	是否有货
5 mg	￥4600	In-stock
10 mg	￥7100	In-stock
25 mg	￥13000	In-stock
50 mg		询价
100 mg		询价

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Glucose Metabolism Compound Library
Anti-Liver Cancer Compound Library
Rare Diseases Drug Library
Anti-Colorectal Cancer Compound Library

生物活性

Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC₅₀ of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies^[1]^[2]^[3].

IC₅₀ & Target^[1]

PI3Kδ

1 nM (IC₅₀)

体外研究
(In Vitro)

Parsaclisib (0.1-3000 nM; 4 d) inhibits proliferation of MCL and DLBCL cell lines^[2].
Parsaclisib (0.1-1000 nM; 2 h) inhibits anti-IgM-induced pAKT (Ser473) in the Ramos Burkitt’s lymphoma cell line, with an IC₅₀ of 1 nM^[2].
Parsaclisib inhibits the proliferation of human, dog, rat, and mouse primary B cells after activation of these receptors, with IC₅₀s ranging from 0.2 to 1.7 nM^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:	Jeko-1, Mino, JVM2, Rec-1, Pfeiffer, SU-DHL-5, SU-DHL-6, WSU-NHL, SU-DHL-4, SU-DHL-8, and WILL-2 cells
Concentration:	0.1-3000 nM
Incubation Time:	4 days
Result:	Resulted in a maximal inhibition of 70-90%, with IC₅₀s of ≤10 nM in the four MCL cell lines. Pfeiffer, SU-DHL-5, SU-DHL-6, and WSU-NHL were highly sensitive, with IC₅₀s from 2 to 8 nM.

体内研究
(In Vivo)

Parsaclisib (10 mg/kg; oral gavage twice daily for 7-19 days) inhibits tumor growth in the BALB/c mice bearing the A20 murine lymphoma cells^[2].
Parsaclisib (0.1-10 mg/kg; p.o. twice daily) slows Pfeiffer xenograft tumor growth in a dose-dependent manner. And Parsaclisib was well tolerated^[2].
Parsaclisib (0.5-1 mg/kg; a single p.o.) inhibits pAKT (Ser473) in Pfeiffer subcutaneous mouse xenograft models^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c mice (5-9 weeks) were inoculated with A20 cells^[2]
Dosage:	10 mg/kg
Administration:	Oral gavage twice daily for 7-19 days
Result:	Resulted in significant tumor growth inhibition (TGI). Reduced the percentage of Tregs (CD4⁺CD25⁺FOXP3⁺) in tumors and spleens. Increased the ratio of CD4⁺ and CD8⁺ T cells to Tregs in spleens and tumors. Decreased the number of CD4⁺CD44^high and CD8⁺CD44^high T cells in both spleens and tumors.

Clinical Trial

分子量

469.34

Formula

C₂₀H₂₃Cl₂FN₆O₂

CAS 号

1995889-48-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

DMSO : 240 mg/mL (511.36 mM; Need ultrasonic)

H₂O : 100 mg/mL (213.07 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1307 mL	10.6533 mL	21.3065 mL
5 mM	0.4261 mL	2.1307 mL	4.2613 mL
10 mM	0.2131 mL	1.0653 mL	2.1307 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 6 mg/mL (12.78 mM); Clear solution

此方案可获得 ≥ 6 mg/mL (12.78 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 60.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 6 mg/mL (12.78 mM); Clear solution

此方案可获得 ≥ 6 mg/mL (12.78 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 60.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 6 mg/mL (12.78 mM); Clear solution

此方案可获得 ≥ 6 mg/mL (12.78 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 60.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Shin N, et al. Abstract 2671: INCB050465, a novel PI3Kδ inhibitor, synergizes with PIM protein kinase inhibition to cause tumor regression in a model of DLBCL. Cancer Research. 2015, Aug. 75(15).

[2]. Shin N, et, al. Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy. J Pharmacol Exp Ther. 2020 Jul;374(1):211-222.

[3]. Yue EW, et, al. INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ). ACS Med Chem Lett. 2019 Oct 17;10(11):1554-1560.

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Ruxolitinib(Synonyms: 芦可替尼; INCB18424)

发表于2024年10月25日由上海金畔生物科技有限公司

Ruxolitinib (Synonyms: 芦可替尼; INCB18424) 纯度: 99.83%

Ruxolitinib (INCB18424) 是有效，选择性的 JAK1/2 抑制剂， IC₅₀ 值分别为 3.3 nM 和 2.8 nM，选择性是 JAK3 的 130 多倍。Ruxolitinib 诱导自噬 (autophagy)，通过毒性线粒体自噬 (mitophagy) 杀死肿瘤细胞。

Ruxolitinib Chemical Structure

CAS No. : 941678-49-5

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥825	In-stock
5 mg	￥750	In-stock
10 mg	￥1100	In-stock
50 mg	￥2800	In-stock
100 mg	￥4500	In-stock
200 mg	￥7200	In-stock
500 mg	￥15000	In-stock
1 g	￥21000	In-stock
5 g		询价
10 g		询价

* Please select Quantity before adding items.

Ruxolitinib 相关产品

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Anti-Blood Cancer Compound Library
Targeted Therapy Drug Library
Mitochondria-Targeted Compound Library
Targeted Diversity Library
Anti-Liver Cancer Compound Library
Rare Diseases Drug Library
Children’s Drug Library

生物活性

Ruxolitinib (INCB18424) is a potent and selective JAK1/2 inhibitor with IC₅₀s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3^[1]. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy^[3].

IC₅₀ & Target^[1]

JAK2

2.8 nM (IC₅₀)

JAK1

3.3 nM (IC₅₀)

Tyk2

19 nM (IC₅₀)

JAK3

428 nM (IC₅₀)

体外研究
(In Vitro)

Ruxolitinib potently and selectively inhibits JAK2V617F-mediated signaling and proliferation, markedly increases apoptosis in a dose dependent manner, and at 64 nM results in a doubling of cells with depolarized mitochondria in Ba/F3 cells.
Ruxolitinib demonstrates remarkable potency against erythroid colony formation with IC₅₀ of 67 nM, and inhibits proliferating of erythroid progenitors from normal donors and polycythemia vera patients with IC₅₀ values of 407 nM and 223 nM, respectively^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ruxolitinib (180 mg/kg, orally, twice a day) results in survive rate of greater than 90% by day 22 and markedly reduces splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminated neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects in a JAK2V617F-driven mouse model^[1].
In the Ruxolitinib group, the primary end point is reached in 41.9% of patients, as compared with 0.7% in the placebo group in the double-blind trial of myelofibrosis. Ruxolitinib results in maintaining of reduction in spleen volume and improvement of 50% or more in the total symptom score^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

306.37

Formula

C₁₇H₁₈N₆

CAS 号

941678-49-5

中文名称

鲁索利替尼；卢索替尼；鲁索替尼；芦可替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (326.40 mM)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2640 mL	16.3201 mL	32.6403 mL
5 mM	0.6528 mL	3.2640 mL	6.5281 mL
10 mM	0.3264 mL	1.6320 mL	3.2640 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 0.5% Methylcellulose/saline water

Solubility: 5 mg/mL (16.32 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 5% DMAC in 0.5% methylcellulose aqueous solution

Solubility: 5 mg/mL (16.32 mM); Suspended solution; Need ultrasonic
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.79 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
4.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.79 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
5.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
6.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117.

[2]. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807.

[3]. Tavallai M, et al. Rationally Repurposing Ruxolitinib (Jakafi (®)) as a Solid Tumor Therapeutic.Front Oncol. 2016 Jun 13;6:142.

Kinase Assay ^[1]	Recombinant proteins are expressed using Sf21 cells and baculovirus vectors and purified with affinity chromatography. JAK kinase assays use a homogeneous time-resolved fluorescence assay with the peptide substrate (-EQEDEPEGDYFEWLE). Each enzyme reaction is carried out with Ruxolitinib or control, JAK enzyme, 500 nM peptide, adenosine triphosphate (ATP; 1mM), and 2% dimethyl sulfoxide (DMSO) for 1 hour. The 50% inhibitory concentration (IC₅₀) is calculated as INCB018424 concentration required for inhibition of 50% of the fluorescent signal. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are seeded at 2×10³/well of white bottom 96-well plates, treated with Ruxolitinib (INCB018424) from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37°C with 5% CO₂. Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values are transformed to percent inhibition relative to vehicle control, and IC₅₀ curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice are fed standard rodent chow and provided with water ad libitum. Ba/F3-JAK2V617F cells (10⁵ per mouse) are inoculated intravenously into 6- to 8-week-old female BALB/c mice. Survival is monitored daily, and moribund mice are humanely killed and considered deceased at time of death. Treatment with vehicle (5% dimethyl acetamide, 0.5% methocellulose) or Ruxolitinib (INCB018424) begin within 24 hours of cell inoculation, twice daily by oral gavage. Hematologic parameters are measured using a Bayer Advia120 analyzed, and statistical significance is determined using Dunnett testing. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117. [2]. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807. [3]. Tavallai M, et al. Rationally Repurposing Ruxolitinib (Jakafi (®)) as a Solid Tumor Therapeutic.Front Oncol. 2016 Jun 13;6:142.

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Pemigatinib(Synonyms: INCB054828)

发表于2024年10月21日由上海金畔生物科技有限公司

Pemigatinib (Synonyms: INCB054828) 纯度: 99.88%

Pemigatinib (INCB054828) 是一种具有口服活性的，选择性 FGFR 抑制剂，对于 FGFR1，FGFR2，FGFR3，FGFR4 的 IC₅₀ 分别为 0.4 nM，0.5 nM，1.2 nM，30 nM。Pemigatinib 有用于胆管癌的潜力。

Pemigatinib Chemical Structure

CAS No. : 1513857-77-6

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Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1290	In-stock
5 mg	￥1200	In-stock
10 mg	￥1900	In-stock
25 mg	￥3500	In-stock
50 mg	￥5500	In-stock
100 mg	￥9500	In-stock
500 mg	￥26500	In-stock
1 g		询价
5 g		询价

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生物活性

Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC₅₀s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma^[1]^[2].

IC₅₀ & Target^[2]

FGFR1

0.4 nM (IC₅₀)

FGFR2

0.5 nM (IC₅₀)

FGFR3

1.2 nM (IC₅₀)

FGFR4

30 nM (IC₅₀)

体外研究
(In Vitro)

This hypothesis is corroborated with in vitro cell-based studies in which cells expressing FGFR2-CLIP1 fusion are sensitive to Pemigatinib (INCB054828; IC₅₀ value of 10.16 nM), whereas cells with the addition of the N549H mutation are resistant to Pemigatinib (IC₅₀ value of 1527.57 nM)^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

487.50

Formula

C₂₄H₂₇F₂N₅O₄

CAS 号

1513857-77-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 25 mg/mL (51.28 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0513 mL	10.2564 mL	20.5128 mL
5 mM	0.4103 mL	2.0513 mL	4.1026 mL
10 mM	0.2051 mL	1.0256 mL	2.0513 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.75 mg/mL (5.64 mM); Clear solution
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: 2.08 mg/mL (4.27 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.27 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.27 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.27 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Arudra K, et al. Calcinosis cutis dermatologic toxicity associated with fibroblast growth factor receptor inhibitor for the treatment of Wilms tumor. J Cutan Pathol. 2018 Oct;45(10):786-790.

[2]. Roskoski R Jr, et al. The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder. Pharmacol Res. 2020 Jan;151:104567.

[3]. Krook MA, et al. Tumor heterogeneity and acquired drug resistance in FGFR2-fusion-positive cholangiocarcinoma through rapid research autopsy. Cold Spring Harb Mol Case Stud. 2019 Aug 1;5(4).

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Epacadostat(Synonyms: INCB 024360)

发表于2024年10月19日由上海金畔生物科技有限公司

Epacadostat (Synonyms: INCB 024360) 纯度: 99.66%

Epacadostat (INCB 024360) 是一种有效，选择性的 IDO1 抑制剂， IC₅₀ 为 71.8 nM。

Epacadostat Chemical Structure

CAS No. : 1204669-58-8

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥675	In-stock
2 mg	￥500	In-stock
5 mg	￥700	In-stock
10 mg	￥1100	In-stock
25 mg	￥1800	In-stock
50 mg	￥2500	In-stock
100 mg	￥4600	In-stock
200 mg	￥8400	In-stock
500 mg		询价
1 g		询价
2 g		询价

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生物活性

Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC₅₀ of 71.8 nM^[1].

IC₅₀ & Target^[1]

IDO1

71.8 nM (IC₅₀)

体外研究
(In Vitro)

In cellular assays, Epacadostat (INCB 024360) selectively inhibits human IDO1 with IC₅₀ values of approximately 10 nM, demonstrating little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). Epacadostat (INCB 024360) also exhibits significant activity toward mouse IDO1, with an IC₅₀ value of 52.4 nM±15.7 nM, in a similar assay using mouse IDO1-transfected HEK293/MSR cells^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Female Balb/c mice bearing CT26 tumors are treated orally twice daily for 12 d with Epacadostat at 100 mg/kg. Epacadostat (INCB 024360) suppresses kynurenine equivalently in plasma, tumors, and lymph nodes. In naïve C57BL/6 mice, 50 mg/kg Epacadostat (INCB 024360) decreases plasma kynurenine levels within 1 hour and those levels stay at least 50% suppressed through the 8-hour time course^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

438.23

Formula

C₁₁H₁₃BrFN₇O₄S

CAS 号

1204669-58-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (228.19 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2819 mL	11.4095 mL	22.8191 mL
5 mM	0.4564 mL	2.2819 mL	4.5638 mL
10 mM	0.2282 mL	1.1410 mL	2.2819 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline

Solubility: ≥ 2.62 mg/mL (5.98 mM); Clear solution
2.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.62 mg/mL (5.98 mM); Clear solution
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.70 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
4.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.70 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
5.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.70 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Liu X, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood. 2010 Apr 29;115(17):3520-30.

[2]. Koblish HK, et al. Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors. Mol Cancer Ther. 2010 Feb;9(2):489-98.

[3]. Fu R, et al. LW106, a novel indoleamine 2,3-dioxygenase 1 inhibitor, suppresses tumour progression by limiting stroma-immune crosstalk and cancer stem cell enrichment in tumour micro-environment. Br J Pharmacol. 2018 Jul;175(14):3034-3049.

Cell Assay ^[1]	To determine Epacadostat activity against IDO in recombinant cells, HEK293/MSR cells are transiently transfected with full-length human or mouse IDO1, or mouse IDO2 cDNA, with Transit-293 transfection reagent or Lipofectamine 2000 reagents. Epacadostat (INCB 024360) at different concentrations is added to the recovered transfected cells seeded at 2×10⁴ cells per well in a 96-well plate (200 μL/well). The cells are incubated for 2 days, and kyn in the supernatants is measured as described in the HeLa cell assay. The tryptophan 2,3-dioxygenase (TDO) assay is performed similarly with HEK293/MSR cells transfected with a human TDO expression vector^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] The female C57BL/6 mice are dosed orally with 50 mg/kg Epacadostat. C57BL/6 wild-type or Ido1^-/--deficient mice are administered a single oral dose of Epacadostat (INCB 024360), at which point food is removed from the cages until after the 8-h time point. At various time points after dosing, mice are euthanized and blood is collected by cardiac puncture. Plasma is analyzed for the presence of Epacadostat (INCB 024360), tryptophan, and kynurenine according to the methods below. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Liu X, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood. 2010 Apr 29;115(17):3520-30. [2]. Koblish HK, et al. Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors. Mol Cancer Ther. 2010 Feb;9(2):489-98. [3]. Fu R, et al. LW106, a novel indoleamine 2,3-dioxygenase 1 inhibitor, suppresses tumour progression by limiting stroma-immune crosstalk and cancer stem cell enrichment in tumour micro-environment. Br J Pharmacol. 2018 Jul;175(14):3034-3049.

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Capmatinib(Synonyms: 卡马替尼; INC280; INCB28060)

发表于2024年10月18日由上海金畔生物科技有限公司

Capmatinib (Synonyms: 卡马替尼; INC280; INCB28060) 纯度: 99.92%

Capmatinib (INC280; INCB28060) 是一种有效的，口服活性的，选择性的，ATP 竞争性的 c-Met 激酶抑制剂 (IC₅₀=0.13 nM)。Capmatinib (INC280; INCB28060) 有效抑制 c-Met 依赖性肿瘤细胞的增殖和迁移，并有效诱导细胞凋亡。抗肿瘤活性。

Capmatinib Chemical Structure

CAS No. : 1029712-80-8

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Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥869	In-stock
5 mg	￥790	In-stock
10 mg	￥950	In-stock
50 mg	￥3100	In-stock
100 mg	￥5500	In-stock
200 mg	￥7700	In-stock
500 mg		询价
1 g		询价

* Please select Quantity before adding items.

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生物活性

Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC₅₀=0.13 nM). Capmatinib (INC280; INCB28060) potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity^[1]^[2].

IC₅₀ & Target

IC50: 0.13 nM (c-MET)^[1]

体外研究
(In Vitro)

Capmatinib (INCB28060) inhibits c-MET phosphorylation with an IC₅₀ value of approximately 1 nM and a concentration of approximately 4 nM inhibits c-MET more than 90%. Capmatinib (INCB28060) inhibits SNU-5 viability or proliferation with an average IC₅₀ value of 1.2 nM and a calculated IC₉₀ value of 4.6 nM Capmatinib (INCB28060) prevents HGF-stimulated H441 cell migration, with IC₅₀ of approximately 2 nM. Again, there is little cell migration at a concentration of 16 nM Capmatinib (INCB28060). Capmatinib (INCB28060) potently and specifically inhibits c-MET enzyme activity, c-MET-mediated signal transduction, and the c-MET-dependent neoplastic phenotype of tumor cells. Capmatinib (INCB28060) exhibits strong antitumor activity in c-MET-dependent tumor models at well-tolerated doses. Capmatinib (INCB28060) exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases. Capmatinib (INCB28060) potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Oral dosing of Capmatinib (INCB28060) results in time- and dose-dependent inhibition of c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models, and the inhibitor is well tolerated at doses that achieve complete tumor inhibition. Furthermore, once daily dosing of 10 mg/kg Capmatinib (INCB28060) results in partial regressions in 6 of 10 U-87MG tumor-bearing mice. It is noted that in both S114 and U-87MG models, tumor growth inhibition increases with increased exposure of the compound and that tumor regressions could only be achieved when the compound exposure consistently exceeded 90% of c-MET inhibition. In these studies, Capmatinib (INCB28060) is well tolerated at all doses during the treatment periods, with no evidence of overt toxicity or weight loss^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

412.42

Formula

C₂₃H₁₇FN₆O

CAS 号

1029712-80-8

中文名称

卡马替尼；苯扎米特

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 25 mg/mL (60.62 mM; Need ultrasonic)

H₂O : 10 mg/mL (24.25 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4247 mL	12.1236 mL	24.2471 mL
5 mM	0.4849 mL	2.4247 mL	4.8494 mL
10 mM	0.2425 mL	1.2124 mL	2.4247 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.04 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.04 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Liu X, et al. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clin Cancer Res. 2011 Nov 15;17(22):7127-38.

[2]. Baltschukat S, et al. Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation. Clin Cancer Res. 2019 May 15;25(10):3164-3175.

Cell Assay ^[1]	Optimal cell density used in the viability assay is predetermined for individual cell lines. To determine compound potency, cells are seeded into 96-well microplates at the appropriate density in media containing 1% to 2% FBS and supplemented with serial dilutions of Capmatinib (INCB28060) in a final volume of 100 μL per well. After 72 hour incubation, 24 μL of CellTiter 96 AQueous One Solution is added to each well, and the plates are incubated for 2 hours in a 37°C incubator. The optical density is measured in the linear range using a microplate reader at 490 nm with wavelength correction at 650 nm. IC₅₀ values are calculated using the GraphPad Prism Software^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Tumor-bearing mice are dosed orally, twice each day with 1, 3, 10, or 30 mg/kg of free base Capmatinib (INCB28060) reconstituted in 5% DMAC in 0.5% methylcellulose for up to 2 weeks. Body weights are monitored throughout the study as a gross measure of toxicity/morbidity. Tumor growth inhibition, expressed in percent, is calculated using the formula: (1−[(volume (treated)/volume (vehicle)])×100. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Liu X, et al. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clin Cancer Res. 2011 Nov 15;17(22):7127-38. [2]. Baltschukat S, et al. Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation. Clin Cancer Res. 2019 May 15;25(10):3164-3175.

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Ruxolitinib phosphate(Synonyms: INCB018424 phosphate)

发表于2024年10月17日由上海金畔生物科技有限公司

Ruxolitinib phosphate (Synonyms: INCB018424 phosphate) 纯度: 99.98%

Ruxolitinib phosphate (INCB018424 phosphate) 是一种有效的 JAK1/2 抑制剂， IC₅₀ 分别为3.3 nM/2.8 nM，比JAK3选择性高130倍。

Ruxolitinib phosphate Chemical Structure

CAS No. : 1092939-17-7

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10 mM * 1 mL in DMSO	￥550	In-stock
5 mg	￥500	In-stock
10 mg	￥700	In-stock
50 mg	￥1700	In-stock
100 mg	￥3100	In-stock
200 mg	￥5800	In-stock
500 mg	￥12000	In-stock
1 g	￥19000	In-stock
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生物活性

Ruxolitinib phosphate (INCB018424 phosphate) is a potent JAK1/2 inhibitor with IC₅₀s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.

IC₅₀ & Target^[1]

JAK2

2.8 nM (IC₅₀)

JAK1

3.3 nM (IC₅₀)

Tyk2

19 nM (IC₅₀)

JAK3

428 nM (IC₅₀)

体外研究
(In Vitro)

Ruxolitinib (INCB018424) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation. Ruxolitinib inhibits the growth of HEL cells with EC₅₀ of 186 nM. Ruxolitinib markedly increases apoptosis in Ba/F3-EpoR-JAK2V617F cell system, and inhibits hematopoietic progenitor cell proliferation in primary MPN patient samples^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ruxolitinib (180 mg/kg, p.o.) reduces the tumor burden of mice inoculated with JAK2V617F-expressing cells without causing anemia or lymphopenia^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

404.36

Formula

C₁₇H₂₁N₆O₄P

CAS 号

1092939-17-7

中文名称

鲁索利替尼磷酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : ≥ 31 mg/mL (76.66 mM)

H₂O : 10 mg/mL (24.73 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4730 mL	12.3652 mL	24.7304 mL
5 mM	0.4946 mL	2.4730 mL	4.9461 mL
10 mM	0.2473 mL	1.2365 mL	2.4730 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 0.5% MC 0.5% Tween-80

Solubility: 10 mg/mL (24.73 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline

Solubility: ≥ 2.75 mg/mL (6.80 mM); Clear solution
3.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.75 mg/mL (6.80 mM); Clear solution
4.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (5.14 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.14 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
5.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.14 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.14 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
6.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.14 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.14 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117.

[2]. Fleischman AG, et al. The CSF3R T618I mutation causes a lethal neutrophilic neoplasia in mice that is responsive to therapeutic JAK inhibition. Blood. 2013 Nov 21;122(22):3628-31.

[3]. de Bock CE, et al. HOXA9 Cooperates with Activated JAK/STAT Signaling to Drive Leukemia Development. Cancer Discov. 2018 May;8(5):616-631.

Cell Assay ^[1]	Cells are seeded at 2000/well of white bottom 96-well plates, treated with compounds from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37°C with 5% CO₂. Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values are transformed to percent inhibition relative to vehicle control, and IC₅₀ curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice are fed standard rodent chow and provided with water ad libitum. Ba/F3-JAK2V617F cells (10⁵ per mouse) are inoculated intravenously into 6- to 8-week-old female BALB/c mice. Survival is monitored daily, and moribund mice are humanely killed and considered deceased at time of death. Treatment with vehicle (5% dimethyl acetamide, 0.5% methocellulose) or Ruxolitinib (INCB018424) begins within 24 hours of cell inoculation, twice daily by oral gavage. Hematologic parameters are measured using a Bayer Advia120 analyzed, and statistical significance is determined using Dunnett testing. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117. [2]. Fleischman AG, et al. The CSF3R T618I mutation causes a lethal neutrophilic neoplasia in mice that is responsive to therapeutic JAK inhibition. Blood. 2013 Nov 21;122(22):3628-31. [3]. de Bock CE, et al. HOXA9 Cooperates with Activated JAK/STAT Signaling to Drive Leukemia Development. Cancer Discov. 2018 May;8(5):616-631.

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Uzansertib phosphate(Synonyms: INCB053914 phosphate)

发表于2024年9月28日由上海金畔生物科技有限公司

Uzansertib phosphate (Synonyms: INCB053914 phosphate) 纯度: 98.44%

Uzansertib (INCB053914) phosphate 是一种具有口服活性的，ATP 竞争性泛-PIM 激酶抑制剂，对于 PIM1，PIM2 和 PIM3 的 IC₅₀ 分别为 0.24 nM，30 nM 和 0.12 nM。Uzansertib phosphate 对多种血液肿瘤细胞系具有广泛的抗增殖活性。

Uzansertib phosphate Chemical Structure

CAS No. : 2088852-47-3

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1 mg	￥1200	In-stock
5 mg	￥3600	In-stock
10 mg	￥5400	In-stock
25 mg	￥9800	In-stock
50 mg	￥15000	In-stock
100 mg		询价
200 mg		询价

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生物活性

Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC₅₀s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines^[1].

IC₅₀ & Target^[1]

PIM1

0.24 nM (IC₅₀)

PIM2

30 nM (IC₅₀)

PIM3

0.12 nM (IC₅₀)

体外研究
(In Vitro)

Uzansertib phosphate inhibits proliferation in all multiple myeloma (MM) cell lines tested, with mean GI₅₀ values ranging from 13.2 nM to 230.0 nM in AML, MM, DLBCL, MCL, and T-ALL cell lines^[1].
Uzansertib phosphate (0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM) inhibits the phosphorylation of downstream PIM kinase substrates (p70S6K/S6 and 4E-BP1) in a dose-dependent manner in MOLM-16 (AML), Pfeiffer (DLBCL), and KMS-12-PE/BM (MM) cell lines^[1].
PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib phosphate (mean IC₅₀, 4 nM and 27 nM, respectively)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Uzansertib phosphate (25-100 mg/kg; PO; twice a day; for 15 days) inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) ^[1].
Uzansertib phosphate demonstrates a dose-dependent inhibition of BAD phosphorylation relative to vehicle at 4 hours post dose (MOLM-16 tumors, IC₅₀=70 nM; KMS-12-BM tumors, IC₅₀=145 nM) ^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female immune compromised (severe combined immunodeficiency [SCID]) mice (5-9 weeks of age) bearing MOLM-16 (AML) or KMS-12-BM (MM)^[1]
Dosage:	25, 50, 75, 100 mg/kg
Administration:	PO; twice a day; for 15 days
Result:	Inhibited tumor growth in a dose-dependent manner in mice.

Clinical Trial

分子量

611.51

Formula

C₂₆H₂₉F₃N₅O₇P

CAS 号

2088852-47-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 5 mg/mL (8.18 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6353 mL	8.1765 mL	16.3530 mL
5 mM	0.3271 mL	1.6353 mL	3.2706 mL
10 mM	—	—	—

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

此方案可获得 ≥ 1.8 mg/mL (2.94 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 18.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

此方案可获得 ≥ 1.8 mg/mL (2.94 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 18.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

此方案可获得 ≥ 1.8 mg/mL (2.94 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 18.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Koblish H, et al. Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies. PLoS One. 2018 Jun 21;13(6):e0199108.

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Itacitinib(Synonyms: INCB039110)

发表于2024年9月17日由上海金畔生物科技有限公司

Itacitinib (Synonyms: INCB039110) 纯度: 99.97%

Itacitinib (INCB039110) 是一种有效的，选择性的 JAK1 抑制剂，对人 JAK1 的 IC₅₀ 值为 2 nM。Itacitinib 对 JAK1 选择性是 JAK2 的 20 多倍，是 JAK3 和 TYK2 的 100 多倍。

Itacitinib Chemical Structure

CAS No. : 1334298-90-6

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥2009	In-stock
5 mg	￥1650	In-stock
10 mg	￥2850	In-stock
50 mg	￥9950	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

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Anti-Blood Cancer Compound Library
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生物活性

Itacitinib (INCB039110) is an orally active and selective inhibitor of JAK1 with an IC₅₀ of 2 nM for human JAK1. Itacitinib shows >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis^[1]^[2].

IC₅₀ & Target^[1]

JAK1

体外研究
(In Vitro)

Itacitinib (INCB039110) is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2. Itacitinib is used in the research of myelofibrosis^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

553.51

Formula

C₂₆H₂₃F₄N₉O

CAS 号

1334298-90-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 30 mg/mL (54.20 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8067 mL	9.0333 mL	18.0665 mL
5 mM	0.3613 mL	1.8067 mL	3.6133 mL
10 mM	0.1807 mL	0.9033 mL	1.8067 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.52 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.52 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.52 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Mascarenhas JO, et al. Primary analysis of a phase II open-label trial of INCB039110, a selective JAK1 inhibitor, in patients with myelofibrosis. Haematologica. 2017 Feb;102(2):327-335.

[2]. Alain Lescoat, et al. Combined Anti-Fibrotic and Anti-Inflammatory Properties of JAK-inhibitors on Macrophages in Vitro and in Vivo: Perspectives for Scleroderma-Associated Interstitial Lung Disease. Biochem Pharmacol. 2020 Jun 17;114103.

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INCB-057643

发表于2024年8月2日由上海金畔生物科技有限公司

INCB-057643 纯度: 98.21%

INCB-057643 是一种新型，口服生物可利用的 BET 抑制剂。

INCB-057643 Chemical Structure

CAS No. : 1820889-23-3

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1737	In-stock
2 mg	￥1100	In-stock
5 mg	￥1900	In-stock
10 mg	￥3200	In-stock
50 mg	￥11500	In-stock
100 mg	￥19500	In-stock
200 mg		询价
500 mg		询价

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生物活性

INCB-057643 is a novel, orally bioavailable BET inhibitor.

IC₅₀ & Target

BET^[1]

体外研究
(In Vitro)

INCB-057643 is a novel, orally bioavailable BET inhibitor. INCB-057643 inhibits binding of BRD2/BRD3/BRD4 to an acetylated histone H4 peptide in the low nM range, and is selective against other bromodomain containing proteins. In vitro analyses show that INCB-057643 inhibits proliferation of human AML, DLBCL, and multiple myeloma cell lines, with a corresponding decrease in MYC protein levels. Cell cycle analyses indicate that G₁ arrest and a concentration-dependent increase in apoptosis are seen within 48 hours of treatment with INCB-057643^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Production of several cytokines, including IL-6, IL-10 and MIP-1α, is repressed by INCB-057643 in human and mouse whole blood stimulated ex vivo with LPS. Oral administration of INCB-057643 results in significant anti-tumor efficacy in xenograft models of AML, myeloma, and DLBCL. Additionally, combining INCB-057643 with standard of care agents used for the treatment of DLBCL including rituximab and bendamustine results in enhanced anti-tumor efficacy relative to that achieved with single agent therapies at doses that are well tolerated^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

415.46

Formula

C₂₀H₂₁N₃O₅S

CAS 号

1820889-23-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (150.44 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4070 mL	12.0349 mL	24.0697 mL
5 mM	0.4814 mL	2.4070 mL	4.8139 mL
10 mM	0.2407 mL	1.2035 mL	2.4070 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.01 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.01 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.01 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Matthew C. Stubbs, et al. Abstract 5071: Preclinical characterization of the potent and selective BET inhibitor INCB057643 in models of hematologic malignancies. AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 5071.

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Parsaclisib(Synonyms: INCB050465)

发表于2024年7月2日由上海金畔生物科技有限公司

Parsaclisib (Synonyms: INCB050465) 纯度: 99.31%

Parsaclisib (INCB050465) 是一种有效，选择性和具有口服活性的 PI3Kδ 抑制剂，IC₅₀ 值为 1 nM。Parsaclisib 相对于其他 PI3K I 类同工型的选择性约为 20000 倍。Parsaclisib 可用于研究复发或难治性 B 细胞恶性肿瘤。

Parsaclisib Chemical Structure

CAS No. : 1426698-88-5

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥5060	In-stock
5 mg	￥4600	In-stock
10 mg	￥7100	In-stock
25 mg	￥13000	In-stock
50 mg		询价
100 mg		询价

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生物活性

Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC₅₀ of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies^[1]^[2]^[3].

IC₅₀ & Target^[1]

PI3Kδ

1 nM (IC₅₀)

体外研究
(In Vitro)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:	Jeko-1, Mino, JVM2, Rec-1, Pfeiffer, SU-DHL-5, SU-DHL-6, WSU-NHL, SU-DHL-4, SU-DHL-8, and WILL-2 cells
Concentration:	0.1-3000 nM
Incubation Time:	4 days
Result:	Resulted in a maximal inhibition of 70-90%, with IC₅₀s of ≤10 nM in the four MCL cell lines. Pfeiffer, SU-DHL-5, SU-DHL-6, and WSU-NHL were highly sensitive, with IC₅₀s from 2 to 8 nM.

体内研究
(In Vivo)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c mice (5-9 weeks) were inoculated with A20 cells^[2]
Dosage:	10 mg/kg
Administration:	Oral gavage twice daily for 7-19 days
Result:	Resulted in significant tumor growth inhibition (TGI). Reduced the percentage of Tregs (CD4⁺CD25⁺FOXP3⁺) in tumors and spleens. Increased the ratio of CD4⁺ and CD8⁺ T cells to Tregs in spleens and tumors. Decreased the number of CD4⁺CD44^high and CD8⁺CD44^high T cells in both spleens and tumors.

Clinical Trial

分子量

432.88

Formula

C₂₀H₂₂ClFN₆O₂

CAS 号

1426698-88-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL (288.76 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3101 mL	11.5505 mL	23.1011 mL
5 mM	0.4620 mL	2.3101 mL	4.6202 mL
10 mM	0.2310 mL	1.1551 mL	2.3101 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline

Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution
2.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.81 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
4.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.81 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
5.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.81 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Niu Shin, et al. Abstract 2671: INCB050465, a novel PI3Kδ inhibitor, synergizes with PIM protein kinase inhibition to cause tumor regression in a model of DLBCL. Cancer Research. 2015, Aug. 75(15).

[2]. Shin N, et, al. Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy. J Pharmacol Exp Ther. 2020 Jul;374(1):211-222.

[3]. Yue EW, et, al. INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ). ACS Med Chem Lett. 2019 Oct 17;10(11):1554-1560.

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INCB059872

发表于2024年5月16日由上海金畔生物科技有限公司

INCB059872

INCB059872是一种有效、具有口服活性，选择性和不可逆的赖氨酸特异性去甲基化酶1 (LSD1) 抑制剂。INCB059872可用于髓系白血病的研究。

INCB059872 Chemical Structure

CAS No. : 1802909-49-4

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 can be used for the research of myeloid leukemia^[1].

IC₅₀ & Target

LSD1^[1]

体外研究
(In Vitro)

INCB059872 (25 nM; 48 hours; 293T cells) increases enhancer activity and gene expression^[1].
INCB059872 (25 nM; 24 hours; THP-1 cells) makes THP-1 show a growth defect within one cell doubling time or approximately 3 days. INCB059872 (100 nM; 24 hours; MV-4–11 cells) treated MV-4–11 cells continues to grow as DMSO-treated cells for multiple cell divisions. INCB059872 (THP-1 cells) regulates PRO-seq analysis identifies genes and enhancers^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	293T cells
Concentration:	250 nM
Incubation Time:	48 hours
Result:	Increased enhancer activity and gene expression.

体内研究
(In Vivo)

INCB059872 (10 mg/kg; p.o.; 0, 4, or 6 days) makes single-cell RNA-seq revealing changes in bone marrow progenitor populations^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice^[1]
Dosage:	10 mg/kg
Administration:	P.o.; 0, 4, or 6 days
Result:	Single-cell RNA-seq revealed changes in bone marrow progenitor populations.

Clinical Trial

分子量

386.53

Formula

C₂₃H₃₄N₂O₃

CAS 号

1802909-49-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Johnston G, et al. Nascent transcript and single-cell RNA-seq analysis defines the mechanism of action of the LSD1 inhibitor INCB059872 in myeloid leukemia. Gene. 2020;752:144758.

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Uzansertib(Synonyms: INCB053914)

发表于2024年5月13日由上海金畔生物科技有限公司

Uzansertib (Synonyms: INCB053914)

Uzansertib (INCB053914) 是一种具有口服活性的，ATP 竞争性泛-PIM 激酶抑制剂，对于 PIM1，PIM2 和 PIM3 的 IC₅₀ 分别为 0.24 nM，30 nM 和 0.12 nM。Uzansertib 对多种血液肿瘤细胞系具有广泛的抗增殖活性。

Uzansertib Chemical Structure

CAS No. : 1620012-39-6

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Uzansertib 的其他形式现货产品:

Uzansertib phosphate

生物活性

Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC₅₀s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines^[1].

IC₅₀ & Target^[1]

PIM1

0.24 nM (IC₅₀)

PIM2

30 nM (IC₅₀)

PIM3

0.12 nM (IC₅₀)

体外研究
(In Vitro)

Uzansertib inhibits proliferation in all multiple myeloma (MM) cell lines tested, with mean GI₅₀ values ranging from 13.2 nM to 230.0 nM in AML, MM, DLBCL, MCL, and T-ALL cell lines^[1].
Uzansertib (0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM) inhibits the phosphorylation of downstream PIM kinase substrates (p70S6K/S6 and 4E-BP1) in a dose-dependent manner in MOLM-16 (AML), Pfeiffer (DLBCL), and KMS-12-PE/BM (MM) cell lines^[1].
PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib (mean IC₅₀, 4 nM and 27 nM, respectively)^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Uzansertib (25-100 mg/kg; PO; twice a day; for 15 days) inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) ^[1].
Uzansertib demonstrates a dose-dependent inhibition of BAD phosphorylation relative to vehicle at 4 hours post dose (MOLM-16 tumors, IC₅₀=70 nM; KMS-12-BM tumors, IC₅₀=145 nM) ^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female immune compromised (severe combined immunodeficiency [SCID]) mice (5-9 weeks of age) bearing MOLM-16 (AML) or KMS-12-BM (MM)^[1]
Dosage:	25, 50, 75, 100 mg/kg
Administration:	PO; twice a day; for 15 days
Result:	Inhibited tumor growth in a dose-dependent manner in mice.

分子量

513.51

Formula

C₂₆H₂₆F₃N₅O₃

CAS 号

1620012-39-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Koblish H, et al. Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies. PLoS One. 2018 Jun 21;13(6):e0199108.

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INCB054329

发表于2024年4月28日由上海金畔生物科技有限公司

INCB054329 纯度: 98.19%

INCB054329 是一种有效的 BET 抑制剂。

INCB054329 Chemical Structure

CAS No. : 1628607-64-6

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥5170	In-stock
5 mg	￥4700	In-stock
10 mg	￥7200	In-stock
25 mg	￥13500	In-stock
50 mg	￥21500	In-stock
100 mg	￥33000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

INCB054329 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
Drug Repurposing Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library

生物活性

INCB054329 is a potent BET inhibitor.

IC₅₀ & Target

BET^[1]

体外研究
(In Vitro)

INCB054329 is a bromodomain and extra-terminal motif (BET) inhibitor^[1]. INCB054329 inhibits binding of BRD2, BRD3 and BRD4 to an acetylated histone H4 peptide with low nanomolar potency. In myeloma cell lines, treatment with INCB054329 inhibits expression of c-MYC and induced HEXIM1. The majority of myeloma, AML, and lymphoma cell lines tested are growth inhibited by INCB054329 with potencies less than 200 nM. Selectivity is seen when compared with nontransformed cells as the potency for growth inhibition of IL-2 stimulated T-cells from normal donors is greater than 1300 nM. Cell cycle analysis reveals treatment-induced G1 arrest. Furthermore in both AML and lymphoma cell lines, INCB054329 induces apoptosis consistent with increased expression of pro-apoptotic regulators^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Oral administration of INCB054329 inhibits tumor growth in several models of hematologic cancers. In the MM1.S multiple myeloma xenograft model, inhibition of tumor growth is correlated with reduction of c-MYC levels. PK-PD analysis shows c-MYC suppression is associated with an IC₅₀ value of less than 100 nM in vivo^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

348.36

Formula

C₁₉H₁₆N₄O₃

CAS 号

1628607-64-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (287.06 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8706 mL	14.3530 mL	28.7059 mL
5 mM	0.5741 mL	2.8706 mL	5.7412 mL
10 mM	0.2871 mL	1.4353 mL	2.8706 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (7.18 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.18 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (7.18 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.18 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (7.18 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Pérez-Salvia M, et al. Bromodomain inhibitors and cancer therapy: From structures to applications. Epigenetics. 2017 May 4;12(5):323-339.

[2]. Phillip CC Liu, et al. Abstract 3523: Discovery of a novel BET inhibitor INCB054329.

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INCB086550(Synonyms: PD-1/PD-L1-IN-8)

发表于2024年3月17日由上海金畔生物科技有限公司

INCB086550 (Synonyms: PD-1/PD-L1-IN-8) 纯度: 98.86%

INCB086550 (PD-1/PD-L1-IN-8; example 24) 是 PD-1/PD-L1 的抑制剂，其IC₅₀ 值为 <= 10 nM。

INCB086550 Chemical Structure

CAS No. : 2230911-59-6

规格	价格	是否有货
5 mg	￥8500	In-stock
10 mg		询价
50 mg		询价

* Please select Quantity before adding items.

INCB086550 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

INCB086550 (PD-1/PD-L1-IN-8; example 24) is a PD-1/PD-L1 inhibitor, with an IC₅₀ <= 10 nM^[1].

分子量

693.79

Formula

C₄₁H₃₉N₇O₄

CAS 号

2230911-59-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

H₂O : 83.33 mg/mL (120.11 mM; ultrasonic and adjust pH to 3 with HCl)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4414 mL	7.2068 mL	14.4136 mL
5 mM	0.2883 mL	1.4414 mL	2.8827 mL
10 mM	0.1441 mL	0.7207 mL	1.4414 mL

参考文献

[1]. WU LIANGXING, et al. BENZOOXAZOLE DERIVATIVES AS IMMUNOMODULATORS. WO2018119266A1.

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Aderbasib(Synonyms: INCB007839; INCB7839)

发表于2024年3月6日由上海金畔生物科技有限公司

Aderbasib (Synonyms: INCB007839; INCB7839) 纯度: 97.07%

Aderbasb (INCB007839) 是一种有效的、具有口服活性的、靶向特异性的低纳摩尔 ADAM10 和 ADAM17 抑制剂。Aderbasb 表现出强大的抗肿瘤活性，可用于癌症研究，包括弥漫性大 B 细胞非霍奇金淋巴瘤，HER2⁺ 乳腺癌，胶质瘤等。

Aderbasib Chemical Structure

CAS No. : 791828-58-5

规格	价格	是否有货
5 mg	￥4000	In-stock
10 mg	￥6500	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

Aderbasib 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
Drug Repurposing Compound Library
Differentiation Inducing Compound Library
Anti-Breast Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library

生物活性

Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2⁺ breast cancer, gliomas, et al^[1].

IC₅₀ & Target^[1]

ADAM10

ADAM17

体外研究
(In Vitro)

Aderbasib inhibits the metalloprotease activity through binding to the active site of the metalloproteinase domain. Aderbasib (10-100 μM) inhibits the interaction between ADAM17 and sE2-Fc, as the concentration of the compound increases, binding of sE2-Fc decreased accordingly, with almost no binding detected at 100 μM in trypsinized PK15 cells^[2].
Aderbasib (100-1000μM; pre-treated for 0.5 h) shows antiviral effect against CSFV pseudovirus at 100 μM and 1 mM in PK15 cells^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Aderbasib (intraperitoneal injection; 50 mg/kg; 5 days per week beginning four weeks; 2 weeks) blocks glioma growth of SU-pcGBM2 NSG mice xenografts^[1].
INCB7839 can be formulated in 2% DMSO, 2% Tween 80, 48% PEG300, 48% water as a injection solution. This is for literature reference only^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NSG mice^[1]
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; 50 mg/kg; 5 days per week beginning four weeks; 2 weeks
Result:	Robustly inhibited growth of pediatric glioblastoma orthotopic xenografts.

Clinical Trial

分子量

416.47

Formula

C₂₁H₂₈N₄O₅

CAS 号

791828-58-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (240.11 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4011 mL	12.0057 mL	24.0113 mL
5 mM	0.4802 mL	2.4011 mL	4.8023 mL
10 mM	0.2401 mL	1.2006 mL	2.4011 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Lois Witters, et al. Synergistic inhibition with a dual epidermal growth factor receptor/HER-2/neu tyrosine kinase inhibitor and a disintegrin and metalloprotease inhibitor. Cancer Res. 2008 Sep 1;68(17):7083-9.

[2]. Fei Yuan, et al. ADAM17 is an essential attachment factor for classical swine fever virus. PLoS Pathog. 2021 Mar 8;17(3):e1009393.

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INCB054329 Racemate

发表于2024年2月12日由上海金畔生物科技有限公司

INCB054329 Racemate

INCB054329 Racemate 是 BET 蛋白的抑制剂。

INCB054329 Racemate Chemical Structure

CAS No. : 1628607-62-4

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

INCB054329 Racemate is a BET protein inhibitor.

IC₅₀ & Target

BET ^[1].

分子量

348.36

Formula

C₁₉H₁₆N₄O₃

CAS 号

1628607-62-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 62.5 mg/mL (179.41 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8706 mL	14.3530 mL	28.7059 mL
5 mM	0.5741 mL	2.8706 mL	5.7412 mL
10 mM	0.2871 mL	1.4353 mL	2.8706 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.97 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.97 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.97 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. ARYL SULFONOHYDRAZIDES. US20160075721.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务