Pralsetinib(Synonyms: 普拉替尼; BLU-667)

发表于2024年10月19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。

Pralsetinib (Synonyms: 普拉替尼; BLU-667) 纯度: 99.98%

Pralsetinib (BLU-667) 是一种高效的选择性 RET 抑制剂。Pralsetinib (BLU-667) 抑制 WT RET，RET 突变体 V804L，V804M，M918T 和 CCDC6-RET 融合，IC₅₀ 分别为 0.4、0.3、0.4、0.4、0.4 nM。

Pralsetinib Chemical Structure

CAS No. : 2097132-94-8

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥2700	In-stock
2 mg	￥1150	In-stock
5 mg	￥2300	In-stock
10 mg	￥3300	In-stock
50 mg	￥9600	In-stock
100 mg		询价

* Please select Quantity before adding items.

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Anti-Lung Cancer Compound Library
Targeted Therapy Drug Library
Anti-Liver Cancer Compound Library
Rare Diseases Drug Library

生物活性

Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC₅₀s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively^[1].

IC₅₀ & Target

IC50: 0.4 nM (Wild type RET), 0.3 nM (RET V804L), 0.4 nM (RET V804M), 0.4 nM (RET M918T), 0.4 nM (CCDC6-RET)^[1]

体外研究
(In Vitro)

Pralsetinib (BLU-667) demonstrates more than 10-fold increased potency over approved MKIs against oncogenic RET variants and resistance mutants^[1].
Pralsetinib (BLU-667) demonstrates potent activity (IC₅₀=0.4 nM) against common oncogenic RET alterations, including RET M918T, an activating mutation found in MTC, as well as the CCDC6-RET fusion observed in PTC and NSCLC^[1].
Pralsetinib (BLU-667) suppresses RET pathway signaling in a panel of RET-driven cell lines: LC2/ad (CCDC6-RET, NSCLC), MZ-CRC-1 (RET M918T, MTC), and TT (RET C634W, MTC)^[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)

Pralsetinib (BLU-667) potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting vascular endothelial growth factor receptor 2 (VEGFR-2)^[1].
Pralsetinib (BLU-667) shows dose dependent activity against both KIF5B-RET Ba/F3 and KIF5B-RET V804L Ba/F3 allograft tumors with doses as low as 10 mg/kg twice-daily^[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

533.60

Formula

C₂₇H₃₂FN₉O₂

CAS 号

2097132-94-8

中文名称

帕拉西替尼；普雷西替尼；普拉替尼；拉西替尼

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 (187.41 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	1.8741 mL	9.3703 mL	18.7406 mL
5 mM	0.3748 mL	1.8741 mL	3.7481 mL
10 mM	0.1874 mL	0.9370 mL	1.8741 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：

——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: ≥ 2.5 mg/mL (4.69 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.69 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% corn oil

Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.69 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。
3.

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

Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

*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]. Subbiah V, et al. Precision Targeted Therapy With BLU-667 for RET-Driven Cancers. American Association for Cancer Research. 10.1158/2159-8290.CD-18-0338.

Cell Assay ^[2]	KIF5B-RET Ba/F3 cells are exposed to compound concentrations ranging from 25 µM to 95.4 pM for 48 hours, and proliferation is assessed with Cell Titer Glo. TT, MZ-CRC-1, TPC-1 or LC2/ad cells are exposed to compound for 4 days and proliferation is measured by BrdU incorporation^[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 Administration ^[2]	Mice^[2] BALB/c nude mice are inoculated subcutaneously into the right flank with KIF5B-RET Ba/F3 cells, KIF5B-RET V804L Ba/F3 cells, or TT cells. For all experiments, mice are dosed twice-daily with vehicle, 3 mg/kg, 10 mg/kg, or 30 mg/kg Pralsetinib (Blu667) or once-daily with 60 mg/kg Pralsetinib (Blu667; administered orally) or 60 mg/kg XL184^[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.
参考文献	[1]. Subbiah V, et al. Precision Targeted Therapy With BLU-667 for RET-Driven Cancers. American Association for Cancer Research. 10.1158/2159-8290.CD-18-0338.

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Avapritinib(Synonyms: BLU-285)

发表于2024年9月22日由上海金畔生物科技有限公司

Avapritinib (Synonyms: BLU-285) 纯度: 99.94%

Avapritinib (BLU-285) 是一种高效、选择性、口服生活性的 KIT 和 PDGFRA 激活环突变激酶抑制剂，其对 KIT D816V 和 PDGFRA D842V 的 IC₅₀ 值分别为 0.27 和 0.24 nM。Avapritinib (BLU-285) 与激酶的活性构象结合，并显示抗肿瘤活性。Avapritinib (BLU-285) 减弱 ABCB1 和 ABCG2 的传输功能。

Avapritinib Chemical Structure

CAS No. : 1703793-34-3

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2303	In-stock
5 mg	￥2100	In-stock
10 mg	￥3500	In-stock
50 mg	￥8900	In-stock
100 mg	￥13000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Avapritinib 相关产品

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Drug Repurposing Compound Library Plus
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Anti-Blood Cancer Compound Library
Targeted Therapy Drug Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library
Rare Diseases Drug Library
Children’s Drug Library

生物活性

Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2^[1]^[2].

IC₅₀ & Target

IC50: 0.27 nM (KIT D816V), 0.24 nM (PDGFRA D842V)^[1]

体外研究
(In Vitro)

Avapritinib (BLU-285) has demonstrated biochemical in vitro activity on the KIT exon 17 mutant enzyme, KIT D816V (IC₅₀=0.27 nM). Cellular activity of Avapritinib on KIT D816 mutants is measured by autophosphorylation in the human mast cell leukemia cell line HMC1.2, and the P815 mouse mastocytoma cell line with IC₅₀=4 and 22 nM, respectively. In Kasumi-1 cells, a t(8;21)-positive AML cell line with a KIT exon 17 N822K mutation, Avapritinib potently inhibits KIT N822K mutant autophosphorylation (IC₅₀=40 nM), downstream signaling, as well as cellular proliferation (IC₅₀=75 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.

体内研究
(In Vivo)

In vivo Avapritinib (BLU-285) is well tolerated and has demonstrated dose dependent antitumor efficacy. Complete tumor growth inhibition and ≥75% KIT kinase inhibition is observed with 10 mg/kg once daily, oral dosing of Avapritinib in the aggressive KIT exon 17 mutant driven P815 mastocytoma model grown as a solid tumor allograft as well as in a disseminated model of disease. Disease burden, measured by whole body luciferase imaging (photons/second/mm²), increases 86-fold in the vehicle control animals over the 24 day dosing period with widespread disease detectable in both femurs, the pelvis and circulating in peripheral blood. Avapritinib at both doses (10 or 30 mg/kg orally, once daily) results in a marked reduction of disease burden throughout the study. Avapritinib at either 10 or 30 mg/kg results in tumor regression in all animals with disease abrogation indistinguishable from background signal measurements in several animals by the end of study. Avapritinib is also well tolerated in this in vivo model and has no adverse effects on body weight at either dose^[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

498.56

Formula

C₂₆H₂₇FN₁₀

CAS 号

1703793-34-3

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 : ≥ 83.33 mg/mL (167.14 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	2.0058 mL	10.0289 mL	20.0578 mL
5 mM	0.4012 mL	2.0058 mL	4.0116 mL
10 mM	0.2006 mL	1.0029 mL	2.0058 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 (5.01 mM); Clear solution

此方案可获得 ≥ 2.5 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 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 (5.01 mM); Clear solution

此方案可获得 ≥ 2.5 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 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 (5.01 mM); Clear solution

此方案可获得 ≥ 2.5 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 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]. Wu CP, et al. Avapritinib: A Selective Inhibitor of KIT and PDGFRα that Reverses ABCB1 and ABCG2-MediatedMultidrug Resistance in Cancer Cell Lines. Mol Pharm. 2019 Jul 1;16(7):3040-3052.

[2]. Evans EK, et al. A precision therapy against cancers driven by KIT/PDGFRA mutations. Sci Transl Med. 2017 Nov 1;9(414). pii: eaao1690.

[3]. Erica Evans, et al. Blu-285, a Potent and Selective Inhibitor for Hematologic Malignancies with KIT Exon 17 Mutations.Blood 2015 126:568.

Animal Administration ^[1]	Mice^[1] A Kasumi-1 luc⁺ AML NOG SCID mouse femoral injection model is used to assess the efficacy of Avapritinib (BLU-285) in KIT exon 17-mutated CBF-AML. Following a 21 day post injection latency period, mice are dosed with Avapritinib orally, once daily at 10 mg/kg or 30 mg/kg through day 45. 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]. Wu CP, et al. Avapritinib: A Selective Inhibitor of KIT and PDGFRα that Reverses ABCB1 and ABCG2-MediatedMultidrug Resistance in Cancer Cell Lines. Mol Pharm. 2019 Jul 1;16(7):3040-3052. [2]. Evans EK, et al. A precision therapy against cancers driven by KIT/PDGFRA mutations. Sci Transl Med. 2017 Nov 1;9(414). pii: eaao1690. [3]. Erica Evans, et al. Blu-285, a Potent and Selective Inhibitor for Hematologic Malignancies with KIT Exon 17 Mutations.Blood 2015 126:568.

Animal Administration
^[1]

Mice^[1]
A Kasumi-1 luc⁺ AML NOG SCID mouse femoral injection model is used to assess the efficacy of Avapritinib (BLU-285) in KIT exon 17-mutated CBF-AML. Following a 21 day post injection latency period, mice are dosed with Avapritinib orally, once daily at 10 mg/kg or 30 mg/kg through day 45.

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]. Wu CP, et al. Avapritinib: A Selective Inhibitor of KIT and PDGFRα that Reverses ABCB1 and ABCG2-MediatedMultidrug Resistance in Cancer Cell Lines. Mol Pharm. 2019 Jul 1;16(7):3040-3052.

[2]. Evans EK, et al. A precision therapy against cancers driven by KIT/PDGFRA mutations. Sci Transl Med. 2017 Nov 1;9(414). pii: eaao1690.

[3]. Erica Evans, et al. Blu-285, a Potent and Selective Inhibitor for Hematologic Malignancies with KIT Exon 17 Mutations.Blood 2015 126:568.

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Fisogatinib(Synonyms: BLU-554)

发表于2024年9月11日由上海金畔生物科技有限公司

Fisogatinib (Synonyms: BLU-554) 纯度: 99.87%

Fisogatinib (BLU-554) 是一种有效的高选择性口服的 FGFR4 抑制剂，其 IC₅₀ 值为 5 nM。Fisogatinib 在依赖 FGFR4 信号传导的肝细胞癌 (HCC) 模型中具有显着的抗肿瘤活性。

Fisogatinib Chemical Structure

CAS No. : 1707289-21-1

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1661	In-stock
5 mg	￥1500	In-stock
10 mg	￥2500	In-stock
50 mg	￥7500	In-stock
100 mg	￥13000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Fisogatinib 相关产品

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Anti-Lung Cancer Compound Library
Angiogenesis Related Compound Library
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生物活性

Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC₅₀ of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling^[1]^[2].

IC₅₀ & Target^[1]

FGFR4

5 nM (IC₅₀)

体内研究
(In Vivo)

Tissue distribution of Fisogatinib (10 mg/kg; oral gavage; for 4 hours; FVB/NRj mice) in wild-type mice is as follows; tissue concentrations decreases in the order liver > kidney > small intestine > spleen > brain. The high Fisogatinib liver-to-plasma ratio suggests there is a relatively high amount of the drug being transported into the liver^[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:	Wild type male mice(FVB/NRj, 11-14 weeks of age)^[1]
Dosage:	10 mg/kg
Administration:	Oral gavage; for 4 hours (Pharmacokinetic study)
Result:	Tissue concentrations decreased in the order liver > kidney > small intestine > spleen > brain.

Clinical Trial

分子量

503.38

Formula

C₂₄H₂₄Cl₂N₄O₄

CAS 号

1707289-21-1

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 (198.66 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9866 mL	9.9329 mL	19.8657 mL
5 mM	0.3973 mL	1.9866 mL	3.9731 mL
10 mM	0.1987 mL	0.9933 mL	1.9866 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 (4.97 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.97 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 (4.97 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.97 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 (4.97 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.97 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 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]. Dogan-Topal B, et al. Quantification of FGFR4 inhibitor BLU-554 in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Mar 15;1110-1111:116-123.

[2]. Richard Kim, et al. First-in-human study of BLU-554, a potent, highly selective FGFR4 inhibitor designed for hepatocellular carcinoma (HCC) with FGFR4 pathway activation. EJC. December 2016, Volume 69, Supplement 1, Page S41.

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BLU9931

发表于2024年5月20日由上海金畔生物科技有限公司

BLU9931 纯度: 99.95%

BLU9931 是一种有效的，高度选择性的，不可逆的成纤维细胞生长因子受体 4 (FGFR4) 抑制剂，其 IC₅₀ 值为 3 nM，K_d 值为 6 nM。BLU9931 具有显着的抗肿瘤活性。

BLU9931 Chemical Structure

CAS No. : 1538604-68-0

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1045	In-stock
5 mg	￥950	In-stock
10 mg	￥1500	In-stock
50 mg	￥3900	In-stock
100 mg	￥6600	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BLU9931 相关产品

•相关化合物库:

Covalent Screening Library Plus
Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Covalent Screening Library
Reprogramming Compound Library
Chemical Probe Library
Anti-Lung Cancer Compound Library
Angiogenesis Related Compound Library
Targeted Diversity Library
Anti-Liver Cancer Compound Library

生物活性

BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC₅₀ of 3 nM and a K_d of 6 nM. BLU9931 has significant antitumor activity^[1].

IC₅₀ & Target

FGFR1

591 nM (IC₅₀)

FGFR2

493 nM (IC₅₀)

FGFR3

150 nM (IC₅₀)

FGFR4

3 nM (IC₅₀)

体外研究
(In Vitro)

BLU9931 inhibits proliferation of HCC cell lines that express an intact FGFR4 signaling complex, with EC₅₀s of 0.07 μM, 0.11 μM and 0.02 μM for Hep 3B, HuH7 and JHH7 cells, respectively^[1].
BLU9931 (0.3-300 nM; 1 hour; MDA-MB-453 and Hep 3B cells) treatment demonstrates potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 cells. BLU9931 shows dose-dependent inhibition of the signaling cascade downstream of FGFR4. BLU9931 exhibits potent inhibition of phosphorylation of the FGFR4 pathway components in Hep 3B cells. BLU9931 treatment leads to induction of caspase-3/7 activity, indicative of induction of apoptosis that results in inhibition of signaling downstream of FGFR4^[1].
BLU9931 (100 nM; 0 -24 hours; Hep 3B cells) treatment increases CYP7A1 mRNA expression and the expression of the proliferative marker EGR1 is inhibited^[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.

Western Blot Analysis^[1]

Cell Line:	MDA-MB-453 and Hep 3B cells
Concentration:	0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
Incubation Time:	1 hour
Result:	Demonstrated potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 and Hep 3B cells.

RT-PCR^[1]

Cell Line:	Hep 3B cells
Concentration:	100 nM
Incubation Time:	0 hour, 4 hours, 8 hour, 24 hours
Result:	Increased CYP7A1 mRNA expression. And the expression of the proliferative marker EGR1 was inhibited.

体内研究
(In Vivo)

BLU9931 (10-100 mg/kg; oral administration; twice every day; for 21 days; mice) treatment demonstrates antitumor activity in HCC xenograft models^[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:	Mice injected with Hep 3B cells^[1]
Dosage:	10 mg/kg, 30 mg/kg or 100 mg/kg
Administration:	Oral administration; twice every day; for 21 days
Result:	Resulted in dose-dependent growth inhibition of Hep 3B tumors. Prevented weight loss in a dose-dependent manner.

分子量

509.38

Formula

C₂₆H₂₂Cl₂N₄O₃

CAS 号

1538604-68-0

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 (245.40 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9632 mL	9.8159 mL	19.6317 mL
5 mM	0.3926 mL	1.9632 mL	3.9263 mL
10 mM	0.1963 mL	0.9816 mL	1.9632 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 (4.08 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.08 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 (4.08 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.08 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 (4.08 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.08 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]. Hagel M, et al. First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov. 2015 Apr;5(4):424-37.

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trans-Pralsetinib(Synonyms: trans-BLU-667)

发表于2024年2月11日由上海金畔生物科技有限公司

trans-Pralsetinib (Synonyms: trans-BLU-667) 纯度: 96.82%

trans-Pralsetinib (trans-BLU-667) 是一个 RET 抑制剂，详细信息请参考专利文献 US20170121312A1 中的化合物 129。

trans-Pralsetinib Chemical Structure

CAS No. : 2097132-93-7

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1530	In-stock
5 mg	￥1300	In-stock
10 mg	￥1850	In-stock
50 mg	￥6850	In-stock
100 mg	￥10800	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

trans-Pralsetinib 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Anti-Lung Cancer Compound Library
Targeted Diversity Library
Anti-Liver Cancer Compound Library

生物活性

trans-Pralsetinib (trans-BLU-667) is a rearranged during transfection (RET) inhibitor extracted from patent US20170121312A1, Compound Example 129^[1].

IC₅₀ & Target

RET^[1]

分子量

533.60

Formula

C₂₇H₃₂FN₉O₂

CAS 号

2097132-93-7

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 (187.41 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8741 mL	9.3703 mL	18.7406 mL
5 mM	0.3748 mL	1.8741 mL	3.7481 mL
10 mM	0.1874 mL	0.9370 mL	1.8741 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: ≥ 4.55 mg/mL (8.53 mM); Clear solution

此方案可获得 ≥ 4.55 mg/mL (8.53 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 45.5 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% corn oil

Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.69 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]. Jason D. Brubaker, et al. Inhibitors of ret. US20170121312A1.

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

BLU-945

发表于2024年2月11日由上海金畔生物科技有限公司

BLU-945

BLU-945 是一种有效的选择性表皮生长因子受体 (EGFR) 抑制剂。EGFR是erbB受体家族的成员，该家族包括跨膜蛋白酪氨酸激酶受体。BLU-945 有效抑制具有 L858R 和/或外显子 19 缺失突变、T790M 突变和 C797S 突变的 EGFR。BLU-945 有助于有效给药并降低 EGFR 介导的靶向毒性。BLU-945 具有研究癌症疾病的潜力 (信息提取自专利 WO2021133809A1，化合物 112)。

BLU-945 Chemical Structure

CAS No. : 2660250-10-0

规格	价格	是否有货
5 mg	￥15200	询问价格 & 货期
10 mg	￥24800	询问价格 & 货期

* Please select Quantity before adding items.

生物活性	receptor (EGFR). EGFR is a member of the erbB receptor family, which includes transmembrane protein tyrosine kinase receptors. BLU-945 effectively inhibits EGFR with L858R and/or exon 19 deletion mutation, T790M mutation, and C797S mutation. BLU-945 facilitates efficacious dosing and reduces EGFR-mediated on-target toxicities. S BLU-945 has the potential for the research of cancer disease (extracted from patent WO2021133809A1, compound 112)^[1].
分子量	556.70
Formula	C₂₈H₃₇FN₆O₃S
CAS 号	2660250-10-0
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]. John Emmerson Campbell, et al. Inhibitors of mutant forms of egfr. Patent WO2021133809A1.

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

whatman (沃特曼)

英国沃特曼 Millipore PALL中国代理商金畔官网

标签归档：blu

Pralsetinib(Synonyms: 普拉替尼; BLU-667)

Pralsetinib 相关产品

•相关化合物库:

Avapritinib(Synonyms: BLU-285)

Avapritinib 相关产品

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Fisogatinib(Synonyms: BLU-554)

Fisogatinib 相关产品

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BLU9931

BLU9931 相关产品

•相关化合物库:

trans-Pralsetinib(Synonyms: trans-BLU-667)

trans-Pralsetinib 相关产品

•相关化合物库:

BLU-945

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