标签归档：cgp

CGP-82996(Synonyms: CINK4)

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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。

CGP-82996 (Synonyms: CINK4)

GP-82996 (CINK4) 是 CDK4/6 的药理学抑制剂。GP-82996 对 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35 的 IC50s 分别为 1.5、5.6 和 25 μM。GP-82996 诱导肿瘤细胞 U2OS 的凋亡 (apoptosis)。GP-82996可用于癌症研究。

CGP-82996(Synonyms: CINK4)

CGP-82996 Chemical Structure

CAS No. : 359886-84-3

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

GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer[1][2].

IC50 & Target[1]

Cdk4/cyclin D1

1.5 μM (IC50)

CDK6/cyclinD1

5.6 μM (IC50)

CDK5/p35

25 μM (IC50)

CDK2/cyclinA

>50 μM (IC50)

CDK1/cyclinB

>100 μM (IC50)

CDK2/cyclin E

>50 μM (IC50)

CDK4/cyclin D2

>50 μM (IC50)

Cdk6/cyclin D2

>50 μM (IC50)

V-abl

>10 μM (IC50)

c-met

>10 μM (IC50)

IGF-1R

>10 μM (IC50)

Insulin-R

>10 μM (IC50)

体外研究
(In Vitro)

GP-82996 (5, 10 μM; 24 hours) induces G1 arrest and G0-G1/S ratio increase in U2OS (p16 negative) and MRC-5 (p16 positive) cells[1].
GP-82996 (5, 10 μM; 24 hours) reduces hyperphosphorylation of pRb, but has no changes in the levels of CDK4 in U2OS, MRC-5 cells[1].
GP-82996 (5, 10 μM; 48 hours) induces aooptosis in 83% of U2OS cells in concentration of 10μM[1].
GP-82996 (0.1-40 μM; 24,48, 72 hours) inhibits the cell proliferation of A549, H358, SKLU-1, H23, PC14 cells with IC50 values of 72 h are 4-7 μM[2].
GP-82996 (3, 5, 10 μM; 48 hours) induces G1 arrest in A549 and H23 cells[2].
GP-82996 ((1, 3, 5, 10 μM; 72 hours) enhances Paclitaxel sensitivity in KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23 cells) [2].
GP-82996 (10 μM; 72 hours) combined with Paclitaxel (3 nM; 72 hours) increases the apoptosis of A549 and H23 cells[2].

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)

GP-82996 (30 mg/kg, i.p. for 29 days) shows smaller final tumor volume compared with vehicle control in mouse xenograft models[1].

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

Animal Model: 19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm3)[1]
Dosage: 30 mg/kg
Administration: i.p. every 12 hours for 29 days
Result: Showed smaller final tumor volume compared with vehicle control in mouse xenograft models.

分子量

456.58

Formula

C27H32N6O
CAS 号

359886-84-3
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.
溶解性数据
In Vivo:
  • 1.

    5% DMSO, 0.05% Tween 80, and 95% physiologic saline
参考文献

  • [1]. Soni R, et al. Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4. J Natl Cancer Inst. 2001 Mar 21;93(6):436-46.

    [2]. Zhang XH, et al. A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS. Cancer Biol Ther. 2013;14(7):597-605.

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

CGP-82996(Synonyms: CINK4)

发表于由
回复

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。

CGP-82996 (Synonyms: CINK4)

GP-82996 (CINK4) 是 CDK4/6 的药理学抑制剂。GP-82996 对 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35 的 IC50s 分别为 1.5、5.6 和 25 μM。GP-82996 诱导肿瘤细胞 U2OS 的凋亡 (apoptosis)。GP-82996可用于癌症研究。

CGP-82996(Synonyms: CINK4)

CGP-82996 Chemical Structure

CAS No. : 359886-84-3

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

GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer[1][2].

IC50 & Target[1]

Cdk4/cyclin D1

1.5 μM (IC50)

CDK6/cyclinD1

5.6 μM (IC50)

CDK5/p35

25 μM (IC50)

CDK2/cyclinA

>50 μM (IC50)

CDK1/cyclinB

>100 μM (IC50)

CDK2/cyclin E

>50 μM (IC50)

CDK4/cyclin D2

>50 μM (IC50)

Cdk6/cyclin D2

>50 μM (IC50)

V-abl

>10 μM (IC50)

c-met

>10 μM (IC50)

IGF-1R

>10 μM (IC50)

Insulin-R

>10 μM (IC50)

体外研究
(In Vitro)

GP-82996 (5, 10 μM; 24 hours) induces G1 arrest and G0-G1/S ratio increase in U2OS (p16 negative) and MRC-5 (p16 positive) cells[1].
GP-82996 (5, 10 μM; 24 hours) reduces hyperphosphorylation of pRb, but has no changes in the levels of CDK4 in U2OS, MRC-5 cells[1].
GP-82996 (5, 10 μM; 48 hours) induces aooptosis in 83% of U2OS cells in concentration of 10μM[1].
GP-82996 (0.1-40 μM; 24,48, 72 hours) inhibits the cell proliferation of A549, H358, SKLU-1, H23, PC14 cells with IC50 values of 72 h are 4-7 μM[2].
GP-82996 (3, 5, 10 μM; 48 hours) induces G1 arrest in A549 and H23 cells[2].
GP-82996 ((1, 3, 5, 10 μM; 72 hours) enhances Paclitaxel sensitivity in KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23 cells) [2].
GP-82996 (10 μM; 72 hours) combined with Paclitaxel (3 nM; 72 hours) increases the apoptosis of A549 and H23 cells[2].

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)

GP-82996 (30 mg/kg, i.p. for 29 days) shows smaller final tumor volume compared with vehicle control in mouse xenograft models[1].

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

Animal Model: 19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm3)[1]
Dosage: 30 mg/kg
Administration: i.p. every 12 hours for 29 days
Result: Showed smaller final tumor volume compared with vehicle control in mouse xenograft models.

分子量

456.58

Formula

C27H32N6O
CAS 号

359886-84-3
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.
溶解性数据
In Vivo:
  • 1.

    5% DMSO, 0.05% Tween 80, and 95% physiologic saline
参考文献

  • [1]. Soni R, et al. Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4. J Natl Cancer Inst. 2001 Mar 21;93(6):436-46.

    [2]. Zhang XH, et al. A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS. Cancer Biol Ther. 2013;14(7):597-605.

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

CGP-82996(Synonyms: CINK4)

发表于由
回复

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。

CGP-82996 (Synonyms: CINK4)

GP-82996 (CINK4) 是 CDK4/6 的药理学抑制剂。GP-82996 对 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35 的 IC50s 分别为 1.5、5.6 和 25 μM。GP-82996 诱导肿瘤细胞 U2OS 的凋亡 (apoptosis)。GP-82996可用于癌症研究。

CGP-82996(Synonyms: CINK4)

CGP-82996 Chemical Structure

CAS No. : 359886-84-3

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

GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer[1][2].

IC50 & Target[1]

Cdk4/cyclin D1

1.5 μM (IC50)

CDK6/cyclinD1

5.6 μM (IC50)

CDK5/p35

25 μM (IC50)

CDK2/cyclinA

>50 μM (IC50)

CDK1/cyclinB

>100 μM (IC50)

CDK2/cyclin E

>50 μM (IC50)

CDK4/cyclin D2

>50 μM (IC50)

Cdk6/cyclin D2

>50 μM (IC50)

V-abl

>10 μM (IC50)

c-met

>10 μM (IC50)

IGF-1R

>10 μM (IC50)

Insulin-R

>10 μM (IC50)

体外研究
(In Vitro)

GP-82996 (5, 10 μM; 24 hours) induces G1 arrest and G0-G1/S ratio increase in U2OS (p16 negative) and MRC-5 (p16 positive) cells[1].
GP-82996 (5, 10 μM; 24 hours) reduces hyperphosphorylation of pRb, but has no changes in the levels of CDK4 in U2OS, MRC-5 cells[1].
GP-82996 (5, 10 μM; 48 hours) induces aooptosis in 83% of U2OS cells in concentration of 10μM[1].
GP-82996 (0.1-40 μM; 24,48, 72 hours) inhibits the cell proliferation of A549, H358, SKLU-1, H23, PC14 cells with IC50 values of 72 h are 4-7 μM[2].
GP-82996 (3, 5, 10 μM; 48 hours) induces G1 arrest in A549 and H23 cells[2].
GP-82996 ((1, 3, 5, 10 μM; 72 hours) enhances Paclitaxel sensitivity in KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23 cells) [2].
GP-82996 (10 μM; 72 hours) combined with Paclitaxel (3 nM; 72 hours) increases the apoptosis of A549 and H23 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)

GP-82996 (30 mg/kg, i.p. for 29 days) shows smaller final tumor volume compared with vehicle control in mouse 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: 19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm3)[1]
Dosage: 30 mg/kg
Administration: i.p. every 12 hours for 29 days
Result: Showed smaller final tumor volume compared with vehicle control in mouse xenograft models.

分子量

456.58

Formula

C27H32N6O
CAS 号

359886-84-3
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.
溶解性数据
In Vivo:
  • 1.

    5% DMSO, 0.05% Tween 80, and 95% physiologic saline
参考文献

  • [1]. Soni R, et al. Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4. J Natl Cancer Inst. 2001 Mar 21;93(6):436-46.

    [2]. Zhang XH, et al. A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS. Cancer Biol Ther. 2013;14(7):597-605.

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

Imatinib carbaldehyde(Synonyms: CGP-57148B carbaldehyde; STI571 carbaldehyde; PROTAC ABL binding moiety 1)

发表于由

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。

Imatinib carbaldehyde (Synonyms: CGP-57148B carbaldehyde; STI571 carbaldehyde; PROTAC ABL binding moiety 1)

Imatinib carbaldehyde (CGP-57148B carbaldehyde) 是一种基于 Imatinib (ABL抑制剂) 的 moiety，可通过 linker 与 IAP 配体结合从而形成 SNIPER 分子。

Imatinib carbaldehyde(Synonyms: CGP-57148B carbaldehyde; STI571 carbaldehyde; PROTAC ABL binding moiety 1)

Imatinib carbaldehyde Chemical Structure

CAS No. : 1436868-85-7

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

Imatinib carbaldehyde (CGP-57148B carbaldehyde), the Imatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER[1].

分子量

507.59

Formula

C29H29N7O2
CAS 号

1436868-85-7
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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

CGP 57380

发表于由

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。

CGP 57380  纯度: 98.0%

CGP 57380 是一种细胞渗透的吡唑-嘧啶类化合物，为具有选择性的 Mnk1 抑制剂，IC50 值为 2.2 μM，但是对 p38，JNK1，ERK1/2，PKC 或 Src-like 激酶等没有抑制作用。

CGP 57380

CGP 57380 Chemical Structure

CAS No. : 522629-08-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1514 In-stock
10 mg ￥1376 In-stock
50 mg ￥5692 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CGP 57380 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Anti-Cancer Compound Library
  • Oxygen Sensing Compound Library
  • Targeted Diversity Library

生物活性

CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.

IC50 & Target[1]

MNK1

2.2 μM (IC50)

体外研究
(In Vitro)

CGP57380 inhibits phosphorylation of eIF4E in cellular assays with IC50 of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells[1]. CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy[2]. CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs)[3]. CGP57380 prevents the serial replating function of BC progenitors[4].

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)

CGP57380 (40 mg/kg/d i.p.) potently extinguishes the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs[4].

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.
分子量

244.23

Formula

C11H9FN6
CAS 号

522629-08-9
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 : 6 mg/mL (24.57 mM; Need ultrasonic and warming)

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

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.0945 mL 20.4725 mL 40.9450 mL
5 mM 0.8189 mL 4.0945 mL 8.1890 mL
10 mM 0.4095 mL 2.0473 mL 4.0945 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 (10.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.24 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 (10.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.24 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
*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]. Knauf U, et al. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol Cell Biol. 2001 Aug;21(16):5500-11.

    [2]. Ishida M, et al. Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ Res. 2003 Dec 12;93(12):1218-24. Epub 2003 Nov 6

    [3]. Chrestensen CA, et al. Loss of MNK function sensitizes fibroblasts to serum-withdrawal induced apoptosis. Genes Cells. 2007 Oct;12(10):1133-40.

    [4]. Lim S, et al. Targeting of the MNK-eIF4E axis in blast crisis chronic myeloid leukemia inhibits leukemia stem cell function. Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):E2298-307
Kinase Assay
[1]

Recombinant p38 isoforms are activated by Mkk6(E) under the following conditions: p38 (100 ng/mL), Mkk6(E) (30 ng/mL), ATP (100 mM) are mixed in kinase buffer (25 mM Hepes, 25 mM b-glycerophosphate, 0.1 mM sodium orthovanadate, 25 mM MgCl2, 2.5 mM DTT, pH 7.4) and incubated for 30 min at 30°C. A typical assay reaction for Mnk1 activity contained Mnk1 (2 ng/mL), HA-eIF4E (10 ng/mL), ATP (300 mM) in kinase buffer. The reaction is started by addition of activated p38 (0.03-3 ng/mL) and stopped after 30 min at 30°C by addition of SDS loading buffer. Inhibitors of Mnk1 are identified under the same assay conditions, except that Mnk1 is pre-activated using active p38a before exposure to the substrate and inhibitors.

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
[4]

CD34+ cells (5×105) or GMPs (1×105) are resuspended in 25 μL 1% FBS/PBS solution and injected into the right femur of 8- to 10-wk-old sublethally irradiated (200 cGy) female mice (n=5 mice per group). Mice injected with 1% FBS/PBS solution serve as a sham control for each experiment. Beginning at 4 wk posttransplantation, mice are monitored for engraftment of human cells by flow cytometry. At 6 wk after transplantation, engrafted mice are treated with vehicle alone, dasatinib (5 mg/kg/d) by gavage, or CGP57380 (40 mg/kg/d) intraperitoneally for 3 wk (n=5 mice per group). At the end of treatment, mice are euthanized, and CD45+ cells are isolated from BM and spleen by using anti-human CD45-specific immunomagnetic microbeads. An aliquot of 1×105 human CD45+ cells is seeded into methylcellulose for the colony forming cell (CFC) assay, and colonies are enumerated after 2 wk. All of the remaining human cells from each primary transplant recipient are then transplanted by intrafemoral injection into secondary recipients, and human engraftment is monitored at 2-wk intervals beginning at 4 wk. At the end of 16 wk, all mice are euthanized. Engraftment in BM and blood is assessed by flow cytometry, and BCR-ABL1 transcripts are detected by RT-PCR.

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]. Knauf U, et al. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol Cell Biol. 2001 Aug;21(16):5500-11.

    [2]. Ishida M, et al. Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ Res. 2003 Dec 12;93(12):1218-24. Epub 2003 Nov 6

    [3]. Chrestensen CA, et al. Loss of MNK function sensitizes fibroblasts to serum-withdrawal induced apoptosis. Genes Cells. 2007 Oct;12(10):1133-40.

    [4]. Lim S, et al. Targeting of the MNK-eIF4E axis in blast crisis chronic myeloid leukemia inhibits leukemia stem cell function. Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):E2298-307

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Midostaurin(Synonyms: 米哚妥林; PKC412; CGP 41251)

发表于由

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。

Midostaurin (Synonyms: 米哚妥林; PKC412; CGP 41251) 纯度: 99.89%

Midostaurin (PKC412; CGP 41251) 是一种多靶点蛋白激酶抑制剂，抑制 PKCα/β/γ，Syk，Flk-1，Akt，PKA，c-Kit，c-Fgr，c-Src，FLT3，PDFRβ 和 VEGFR1/2 的 IC50 值范围为 22-500 nM。

Midostaurin(Synonyms: 米哚妥林; PKC412; CGP 41251)

Midostaurin Chemical Structure

CAS No. : 120685-11-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2260 In-stock
1 mg ￥770 In-stock
5 mg ￥1800 In-stock
10 mg ￥2880 In-stock
50 mg ￥7500 In-stock
100 mg ￥12000 In-stock
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生物活性

Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM[1][2].

IC50 & Target

nPKC-η

160 nM (IC50)

cPKC-α

22 nM (IC50)

cPKC-γ

24 nM (IC50)

cPKC-β1

30 nM (IC50)

cPKC-β2

31 nM (IC50)

nPKC-δ

33 nM (IC50)

nPKC-ε

1250 nM (IC50)

aPKC-ζ

465000 nM (IC50)

PPK

38 nM (IC50)

KDR

86 nM (IC50)

c-Syk

95 nM (IC50)

cdk1/cycB

570 nM (IC50)

Protein kinase A

570 nM (IC50)

c-Fgr

790 nM (IC50)

c-Src

800 nM (IC50)

Flt-1

912 nM (IC50)

EGF-R

1100 nM (IC50)

Myosin-light chain kinase

1900 nM (IC50)

Flk-1

3900 nM (IC50)

c-Lyn

4300 nM (IC50)

P70S6 kinase

5000 nM (IC50)

CSK

8000 nM (IC50)

体外研究
(In Vitro)

Midostaurin (PKC412) shows a broad antiproliferative activity against various tumor and normal cell lines in vitro, and is able to reverse the Pgp-mediated multidrug resistance of tumor cells in vitro. Exposure of cells to Midostaurin (PKC412) results in a dose-dependent increase in the G2/M phase of the cell cycle concomitant with increased polyploidy, apoptosis and enhanced sensitivity to ionizing radiation[1]. Midostaurin (PKC412) induces substantial inhibition of KIT-, Lyn-, and STAT5 activity, but does not suppress Btk in HMC-1 cells and primary neoplastic mast cells[3]. Midostaurin (PKC412) inhibits EN fusion tyrosine kinase in hematopoietic Ba/F3 cells. Midostaurin (PKC412) significantly inhibits EN phosphorylation in M0-91 and IMS-M2 cells in a dose-dependent manner[4].

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)

Midostaurin (PKC412) strongly inhibits retinal neovascularization as well as laser-induced choroidal neovascularization in murine models[1]. Midostaurin (PKC412) (25 mg/kg, i.p.) protects mouse livers of the K18 Arg90Cys-overexpressing transgenic mice from Fas-induced apoptosis[5].

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

570.64

Formula

C35H30N4O4
CAS 号

120685-11-2
中文名称

米哚妥林
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°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 : 50 mg/mL (87.62 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7524 mL 8.7621 mL 17.5242 mL
5 mM 0.3505 mL 1.7524 mL 3.5048 mL
10 mM 0.1752 mL 0.8762 mL 1.7524 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：

——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 (4.38 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.38 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 (4.38 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.38 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]. Fabbro D, et al. PKC412–a protein kinase inhibitor with a broad therapeutic potential. Anticancer Drug Des. 2000 Feb;15(1):17-28.

    [2]. Fabbro D, et al. Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent. Pharmacol Ther. 1999 May-Jun;82(2-3):293-301.

    [3]. Gleixner KV, et al. Synergistic growth-inhibitory effects of Midostaurin (PKC412) on neoplastic mast cells carrying KIT D816V. Haematologica. 2013 Sep;98(9):1450-7.

    [4]. Chi HT, et al. ETV6-NTRK3 as a therapeutic target of small molecule inhibitor PKC412. Biochem Biophys Res Commun. 2012 Dec 7;429(1-2):87-92.

    [5]. Kwan R, et al. PKC412 normalizes mutation-related keratin filament disruption and hepatic injury in mice by promoting keratin-myosin binding. Hepatology. 2015 Dec;62(6):1858-69.
Cell Assay
[3]

Proliferation is determined by trypan blue dye exclusion test. Cells in suspension are seeded in six-well plates at a density of 1×105 cells/mL in the presence of different concentrations of PKC412 for 3 days. In control wells, DMSO instead of Midostaurin (PKC412) is added. After the treatment, 10 μL of the cell suspension is mixed with 10 μL of 0.4% trypan blue, and alive cells are counted manually using a hemacytometer. Results are calculated as the percentage of the values measured when cells are grown in the absence of the reagent. All experiments are performed in triplicate[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.
Animal Administration
[4]

K8-deficient, K18-deficient, and human K18 R90C-overexpressing mice with age of 6-8 weeks are used in the assay. Age and sex matched mice are treated with Midostaurin (25 mg/kg), daily for 4 d or with an equal volume of DMSO as vehicle (both administered intraperitoneally). On day 5 post-treatment, apoptosis is induced by intraperitoneal injection of Fas ligand (Fas-L) (0.15 μg/g body weight). Mice are fasted overnight before Fas Ab injection, and 18 mice are used per DMSO or Midostaurin (PKC412) group for the Fas-treated mice while 6 mice are used per DMSO or Midostaurin (PKC412) group for the control non-Fas-treated mice. Mice are sacrificed by CO2 inhalation 6 h after Fas Ab injection. Blood is collected by intracardiac puncture, and livers are harvested for hematoxylin and eosin (HE) staining (after fixation in 10% formalin) or frozen in optimum cutting temperature compound for immunofluorescence staining[4].

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]. Fabbro D, et al. PKC412–a protein kinase inhibitor with a broad therapeutic potential. Anticancer Drug Des. 2000 Feb;15(1):17-28.

    [2]. Fabbro D, et al. Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent. Pharmacol Ther. 1999 May-Jun;82(2-3):293-301.

    [3]. Gleixner KV, et al. Synergistic growth-inhibitory effects of Midostaurin (PKC412) on neoplastic mast cells carrying KIT D816V. Haematologica. 2013 Sep;98(9):1450-7.

    [4]. Chi HT, et al. ETV6-NTRK3 as a therapeutic target of small molecule inhibitor PKC412. Biochem Biophys Res Commun. 2012 Dec 7;429(1-2):87-92.

    [5]. Kwan R, et al. PKC412 normalizes mutation-related keratin filament disruption and hepatic injury in mice by promoting keratin-myosin binding. Hepatology. 2015 Dec;62(6):1858-69.

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O-Desmethyl Midostaurin(Synonyms: CGP62221; O-Desmethyl PKC412)

发表于由

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。

O-Desmethyl Midostaurin (Synonyms: CGP62221; O-Desmethyl PKC412) 纯度: 95.48%

O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) 是 Midostaurin (HY-10230) 的活性代谢物，通过细胞色素 P450 肝酶代谢产生，可以作为 Midostaurin 在体内代谢的指标之一。Midostaurin 是一种多靶点蛋白激酶 (kinase) 抑制剂，IC50 范围为 22-500 nM。

O-Desmethyl Midostaurin(Synonyms: CGP62221; O-Desmethyl PKC412)

O-Desmethyl Midostaurin Chemical Structure

CAS No. : 740816-86-8

规格 价格 是否有货 数量
5 mg ￥18500 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

生物活性

O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo[1]. Midostaurin is a multi-targeted protein kinase inhibitor with IC50 ranging from 22-500 nM.

IC50 & Target

IC50: active metabolite of Midostaurin[1]
分子量

556.61

Formula

C34H28N4O4
CAS 号

740816-86-8
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
参考文献

  • [1]. Levis M, et al. Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors.Blood. 2006 Nov 15;108(10):3477-83.

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PCR板硅胶片适用于96孔PCR板CGP-9-W-

发表于由

PCR板硅胶片适用于96孔PCR板

  • 产品型号：CGP-9-W-
  • 简要描述：PCR板硅胶片适用于96孔PCR板上海金畔生物科技有限公司供应：全系荧光定量PCR耗材，移液器吸嘴，离心管，冻存管，培养皿，培养板，培养瓶，吸头，仪器及手套，色谱耗材，针头过滤器。
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  • 产品简介

PCR板硅胶片适用于96孔PCR板上海金畔生物科技有限公司供应：移液器吸嘴，离心管，冻存管，培养皿，全系荧光定量PCR耗材。

PCR板硅胶片

订货号 描述
SR6590 进口PCR板封膜超薄透明，可用于荧光定量qPCR
CGP-9-W- PCR板硅胶片，适用于96孔PCR板，“-”开口，白色
CGP-9-WS- PCR板硅胶片，适用于96孔PCR板，“-”开口，白色，灭菌
CGP-9-IMP-W- PCR板硅胶片，适用于96孔PCR板，“-”开口，白色，化学耐受型
CGP-9-IMP-WS- PCR板硅胶片，适用于96孔PCR板，“-”开口，白色，灭菌，化学耐受型
CGD-3-W+ PCR板硅胶片，适用于384孔PCR板，“+”开口，圆形孔
CGD-3-WS+ PCR板硅胶片，适用于384孔PCR板，“+”开口，圆形孔，灭菌
CGD-3-IMP-W+ PCR板硅胶片，适用于384孔PCR板，“+”开口，圆形孔，化学耐受型
CGD-3-IMP-WS+ PCR板硅胶片，适用于384孔PCR板，“+”开口，圆形孔，灭菌，化学耐受型

PCR板硅胶片适用于96孔PCR板适应客户：医院检验科PCR实验室，中心实验室，肝病中心；第三方检测机构，科研院所，大专院校，制药厂，试剂生产厂家，疾控中心，检验检疫。 

CGP37157

发表于由

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。

CGP37157  纯度: 99.77%

CGP37157 是一种 Na+/Ca2+ exchanger 抑制剂，可抑制豚鼠心脏线粒体 Na+ 诱导的 Ca2+ 的释放，IC50 值为 0.8 μM。

CGP37157

CGP37157 Chemical Structure

CAS No. : 75450-34-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550 In-stock
5 mg ￥500 In-stock
10 mg ￥850 In-stock
25 mg ￥1700 In-stock
50 mg ￥2850 In-stock
100 mg ￥4850 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CGP37157 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
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  • Targeted Diversity Library

生物活性

CGP37157 is a potent, selective inhibitor of Na+/Ca2+ exchanger, inhibiting the Na+-induced Ca2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM.

IC50 & Target

IC50: 0.8 μM (Na+/Ca2+ exchanger)[1]
体外研究
(In Vitro)

CGP37157 (Compound XVI) is a potent, selective inhibitor of Na+/Ca2+ exchanger, inhibiting the Na+-induced Ca2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM[1]. CGP37157 (10 μM) shows inhibitory effect on mitochondrial Na+/Ca2+ exchanger in cortical neurons, modulates intracellular Ca2+ levels via suppresssing voltage-gated calcium channels, and reduces NMDA-induced cytosolic and mitochondrial Ca2+ overloads. CGP37157 (10 μM) also reduces NMDA-induced excitotoxicity, and such an effect is via attenuating mitochondrial damage and calpain activity in neurons[2]. CGP37157 (10 μM) in combination with salinomycin significantly attenuates cell viability and increases apoptosis of FaDu and HLaC79 cells. Moreover, CGP37157 has no inhibitory effect on salinomycin tumor toxicity[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.
分子量

324.22

Formula

C15H11Cl2NOS
CAS 号

75450-34-9
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 (385.54 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 3.0843 mL 15.4216 mL 30.8433 mL
5 mM 0.6169 mL 3.0843 mL 6.1687 mL
10 mM 0.3084 mL 1.5422 mL 3.0843 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 (7.71 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.71 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 (7.71 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.71 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]. Chiesi M, et al. Structural dependency of the inhibitory action of benzodiazepines and related compounds on the mitochondrial Na+-Ca2+ exchanger. Biochem Pharmacol. 1988 Nov 15;37(22):4399-403.

    [2]. Ruiz A, et al. CGP37157, an inhibitor of the mitochondrial Na+/Ca2+ exchanger, protects neurons from excitotoxicity by blocking voltage-gated Ca2+ channels. Cell Death Dis. 2014 Apr 10;5:e1156.

    [3]. Scherzed A, et al. Effects of salinomycin and CGP37157 on head and neck squamous cell carcinoma cell lines in vitro. Mol Med Rep. 2015 Sep;12(3):4455-61.
Cell Assay
[1]

Cell toxicity assays are performed. Neurons are exposed to NMDA in HBSS (free of Ca2+ and Mg2+) containing 2.6 mM CaCl2, 10 mM glucose and 10 μM glycine for 10 or 30 min at 37°C, depending on the experiment. CGP37157 is present before and during the excitotoxic insult and cell viability is assessed 24 h later using Citotox 96 colorimetric assay. All experiments are performed in quadruplicate and the values provided are the normalized mean ± S.E.M. of at least three independent experiments[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]. Chiesi M, et al. Structural dependency of the inhibitory action of benzodiazepines and related compounds on the mitochondrial Na+-Ca2+ exchanger. Biochem Pharmacol. 1988 Nov 15;37(22):4399-403.

    [2]. Ruiz A, et al. CGP37157, an inhibitor of the mitochondrial Na+/Ca2+ exchanger, protects neurons from excitotoxicity by blocking voltage-gated Ca2+ channels. Cell Death Dis. 2014 Apr 10;5:e1156.

    [3]. Scherzed A, et al. Effects of salinomycin and CGP37157 on head and neck squamous cell carcinoma cell lines in vitro. Mol Med Rep. 2015 Sep;12(3):4455-61.

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Aliskiren hemifumarate(Synonyms: 阿利克仑半富马酸盐; CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate)

发表于由

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。

Aliskiren hemifumarate (Synonyms: 阿利克仑半富马酸盐; CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate) 纯度: 98.98%

Aliskiren hemifumarate (CGP 60536 hemifumarate) 是肾素的直接抑制剂，IC50为1.5 nM。

Aliskiren hemifumarate(Synonyms: 阿利克仑半富马酸盐; CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate)

Aliskiren hemifumarate Chemical Structure

CAS No. : 173334-58-2

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in Water ￥698 In-stock
10 mg ￥520 In-stock
50 mg ￥1100 In-stock
100 mg ￥1800 In-stock
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500 mg   询价  

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  • Rare Diseases Drug Library

生物活性

Aliskiren hemifumarate(CGP 60536 hemifumarate) is a direct renin inhibitor with IC50 of 1.5 nM. IC50 value: 1.5 nM [1] Target: renin in vitro: Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin. Oral bioavailability of Aliskiren hemifumarate is 2.4% in rats, 16% in marmosets and about 2.5% in humans [2]. in vivo: Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets[3].Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension[4].

Clinical Trial

分子量

1219.59

Formula

C64H110N6O16
CAS 号

173334-58-2
中文名称

阿利克仑半富马酸盐
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: 

H2O : ≥ 50 mg/mL (41.00 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 0.8199 mL 4.0997 mL 8.1995 mL
5 mM 0.1640 mL 0.8199 mL 1.6399 mL
10 mM 0.0820 mL 0.4100 mL 0.8199 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。
参考文献

  • [1]. Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACS Med. Chem. Lett., 2012, 3 (9), pp 754-758

    [2]. Buczko W, et al. Pharmacokinetics and pharmacodynamics of aliskiren, an oral direct renin inhibitor. Pharmacol Rep. 2008 Sep-Oct;60(5):623-31.

    [3]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor.Biochem Biophys Res Commun, 2003, 308(4), 698-705.

    [4]. Gradman AH, et al.Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation, 2005, 111(8), 1012-1018.

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Aliskiren(Synonyms: 阿利克仑; CGP 60536; CGP60536B; SPP 100)

发表于由

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。

Aliskiren (Synonyms: 阿利克仑; CGP 60536; CGP60536B; SPP 100) 纯度: 99.16%

Aliskiren(CGP 60536)是肾素抑制剂，IC50为1.5 nM。

Aliskiren(Synonyms: 阿利克仑; CGP 60536; CGP60536B; SPP 100)

Aliskiren Chemical Structure

CAS No. : 173334-57-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1105 In-stock
5 mg ￥910 In-stock
10 mg ￥1450 In-stock
50 mg ￥2900 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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  • Drug-Induced Liver Injury (DILI) Compound Library
  • Rare Diseases Drug Library

生物活性

Aliskiren(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM. IC50 value: 1.5 nM [1] Target: renin in vitro: Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin. Oral bioavailability of Aliskiren hemifumarate is 2.4% in rats, 16% in marmosets and about 2.5% in humans [2]. in vivo: Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets[3].Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension[4].

Clinical Trial

分子量

551.76

Formula

C30H53N3O6
CAS 号

173334-57-1
中文名称

阿利吉仑；阿利克仑；阿立克仑
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -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: 

Ethanol : 100 mg/mL (181.24 mM; Need ultrasonic)

DMSO : 100 mg/mL (181.24 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8124 mL 9.0619 mL 18.1238 mL
5 mM 0.3625 mL 1.8124 mL 3.6248 mL
10 mM 0.1812 mL 0.9062 mL 1.8124 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 (4.53 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.53 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 (4.53 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.53 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 (4.53 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.53 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]. Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACS Med. Chem. Lett., 2012, 3 (9), pp 754–758

    [2]. Chang AY, et al. Interplay between brain stem angiotensins and monocyte chemoattractant protein-1 as a novel mechanism for pressor response after ischemic stroke. Neurobiol Dis. 2014 Nov;71:292-304.

    [3]. Buczko W, et al. Pharmacokinetics and pharmacodynamics of aliskiren, an oral direct renin inhibitor. Pharmacol Rep. 2008 Sep-Oct;60(5):623-31.

    [4]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor.Biochem Biophys Res Commun, 2003, 308(4), 698-705.

    [5]. Gradman AH, et al.Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation, 2005, 111(8), 1012-1018.

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CGP60474

发表于由

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。

CGP60474  纯度: 98.70%

CGP60474 是一种高效的抗内毒素药物，是一种有效的细胞周期蛋白依赖激酶 (CDK) 抑制剂 (CDK1/B、CDK2/E、CDK2/a、CDK4/D、CDK5/p25、CDK7/H 和 CDK9/T 的 IC50 值分别为 26、3、4、216、10、200 和 13 nM)。CGP60474 是一种选择性和 ATP 竞争性 PKC 抑制剂。

CGP60474

CGP60474 Chemical Structure

CAS No. : 164658-13-3

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1210 In-stock
5 mg ￥1100 In-stock
10 mg ￥1720 In-stock
50 mg ￥6400 In-stock
100 mg ￥8500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor[1][2][3].

IC50 & Target

PKC

 

CDK1-Cyclin B

26 nM (IC50)

CDK2/cyclinE

3 nM (IC50)

cdk2/cyclin A

4 nM (IC50)

Cdk5/p25

10 nM (IC50)

CDK7/cyclin H

200 nM (IC50)

CDK9/cycT

13 nM (IC50)

CDK4/cyclin D

216 nM (IC50)

体外研究
(In Vitro)

CGP60474 (Compound A) is a potent VEGFR-2 inhibitor, with an IC50 of 84 nM[1]. CGP60474 is also a PKC inhibitor, with competitive kinetics relative to ATP[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)

CGP-60474 (10 mg/kg; i.p.) inhibits the IL-6 level and increases the survival rate in the LPS endotoxemia model[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: C57Bl/6 mice (LPS endotoxemia model)[2]
Dosage: 10 mg/kg
Administration: I.p.
Result: Had a higher survival rate.

分子量

355.82

Formula

C18H18ClN5O
CAS 号

164658-13-3
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 : ≥ 50 mg/mL (140.52 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 2.8104 mL 14.0520 mL 28.1041 mL
5 mM 0.5621 mL 2.8104 mL 5.6208 mL
10 mM 0.2810 mL 1.4052 mL 2.8104 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 (7.03 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.03 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 (7.03 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.03 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]. Jorda R, et al. How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?. J Med Chem. 2018;61(20):9105-9120.

    [2]. Han HW, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. Sci Rep. 2018;8(1):14969. Published 2018 Oct 8.

    [3]. Stanetty P, et al. Novel and efficient access to phenylamino-pyrimidine type protein kinase C inhibitors utilizing a Negishi cross-coupling strategy. J Org Chem. 2005;70(13):5215-5220.

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CGP52411(Synonyms: DAPH)

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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。

CGP52411 (Synonyms: DAPH)

CGP52411 (DAPH) 是一种高选择性，有效，口服活性和 ATP 竞争性的 EGFR 抑制剂，IC50 为 0.3 μM。CGP52411 阻止有毒的 Ca2+ 离子流入神经元细胞，并显着抑制和逆转与阿尔茨海默症相关的 β-amyloid (Aβ42) 原纤维聚集物的形成。

CGP52411(Synonyms: DAPH)

CGP52411 Chemical Structure

CAS No. : 145915-58-8

规格 价格 是否有货
5 mg ￥6600 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer’s disease[1][2].

IC50 & Target[1][2]

EGFR

0.3 μM (IC50)

Amyloid-β

 

体外研究
(In Vitro)

CGP52411 (DAPH; 0-100 μM; 90 minutes; A431 cells) treatment inhibits autophosphorylation and c-src autophosphorylation in vitro in a dose-dependent manner with IC50s of 1 μM and 16 μM, respectively. CGP52411 treatment also shows a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2 with an IC50 value of 10 μM[1].
CGP52411 (DAPH) inhibits c-src kinase with an IC50 value of 16 μM. CGP52411 inhibits PKC isozymes isolated from porcine brain with an IC50 of 80 μM. CGP52411 inhibits conventional PKC isozymes (cPKCs α, β-1, β-2, and γ) but not nonconventional PKC isozymes (nPKCs δ, ε, and ζ) or atypical PKC isozymes (aPKC η)[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: A431 cells
Concentration: 0 μM, 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM
Incubation Time: 90 minutes
Result: Inhibited autophosphorylation in vitro in a dose-dependent manner with an IC50 of 1 μM. c-src autophosphorylation was inhibited with an IC50 of 16 μM. And also resulted in a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2, with an estimated IC50 value of 10 μM.

体内研究
(In Vivo)

CGP52411 (3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg; oral administration; daily; for 15 days; female BALB/c nude mice) treatment in vivo against xenografts of the A431 and SK-OV-3 tumors, and has antitumor activity[1].

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

Animal Model: Female BALB/c nude mice injected with A431cells[1]
Dosage: 3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg
Administration: Oral administration; daily; for 15 days
Result: Antitumor efficacy was obtained at doses between 50 mg/kg and 6.3 mg/kg.

分子量

329.35

Formula

C20H15N3O2
CAS 号

145915-58-8
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
参考文献

  • [1]. Buchdunger E, et al. 4,5-Dianilinophthalimide: a protein-tyrosine kinase inhibitor with selectivity for the epidermal growth factor receptor signal transduction pathway and potent in vivo antitumor activity. Proc Natl Acad Sci U S A. 1994 Mar 15;91(6):2334-8.

    [2]. Blanchard BJ, et al. Efficient reversal of Alzheimer’s disease fibril formation and elimination of neurotoxicity by a small molecule. Proc Natl Acad Sci U S A. 2004 Oct 5;101(40):14326-32.

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适用于96孔PCR板,白色,无菌CGP-9-W-

发表于由

适用于96孔PCR板,白色,无菌

  • 产品型号：CGP-9-W-
  • 简要描述：适用于96孔PCR板,白色,无菌上海金畔生物科技有限公司供应：光度计，检测仪，免疫仪，全系荧光定量PCR耗材，移液器，钻石吸嘴，离心管，冻存管，培养皿，培养板，培养瓶，吸头，仪器及手套，色谱耗材，针头过滤器。
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  • 产品简介

适用于96孔PCR板,白色,无菌上海金畔生物科技有限公司供应：光度计，检测仪，移液器，钻石吸嘴，离心管，冻存管，培养皿，全系荧光定量PCR耗材。

PCR 板      

CGP-9-W- PCR板硅胶片，适用于96孔PCR板，“-”开口，白色

CGP-9-WS- PCR板硅胶片，适用于96孔PCR板，“-”开口，白色，灭菌

CGP-9-IMP-W- PCR板硅胶片，适用于96孔PCR板，“-”开口，白色，化学耐受型

CGP-9-IMP-WS- PCR板硅胶片，适用于96孔PCR板，“-”开口，白色，灭菌，化学耐受型

包装规格  ： 10片/袋，5袋/箱(50片/箱）

适用于96孔PCR板,白色,无菌CGP-9-W-

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CG-0020预组装黑色实心盖； PTFE/硅胶垫

产品优势：金畔生物代理实验室耗材,PCR耗材品种全，可替代仪器原厂耗材，性价比高，质量稳定，对用户可以节省实验成本。
适应客户：医院检验科PCR实验室，中心实验室，肝病中心；第三方检测机构，科研院所，大专院校，制药厂，试剂生产厂家，疾控中心，检验检疫。 

温馨提示：不可用于临床治疗。

CGP77675

发表于由

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。

CGP77675  纯度: 98.85%

CGP77675 是一种口服有效的 Src 家族激酶抑制剂。CGP77675 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC50 分别为 5-20 和 40 nM)，并且还抑制 Src，EGFR，KDR，v-Abl 和 Lck，IC50 分别为 20、150、1000、310 和 290 nM。具有抗肿瘤活性。

CGP77675

CGP77675 Chemical Structure

CAS No. : 234772-64-6

规格 价格 是否有货 数量
5 mg ￥5500 In-stock
10 mg ￥8250 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

CGP77675 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity[1].

IC50 & Target

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]
体外研究
(In Vitro)

CGP77675 dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC50 value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC50 value of 16.7 nM. These IC50 values are similar to the value obtained with chicken Src (20 nM)[1].
CGP77675 inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC50 of 0.8 μM[1].
CGP77675 (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC50 values 0.2, 0.5, and 5.7μM) in IC8.1 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.

Cell Viability Assay[1]

Cell Line: MC3T3-E1 cells
Concentration: 0.2, 1, and 5 μM
Incubation Time: 3 days
Result: Did not influence cell viability for up to 3 days of treatment.

Western Blot Analysis[1]

Cell Line: Src-overexpressing IC8.1 cells
Concentration: 0.04, 0.2, 1, 5, and 10 μM
Incubation Time: 2 hours
Result: Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.

体内研究
(In Vivo)

CGP77675 (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice[1].
CGP77675 (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats[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: Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1]
Dosage: 1, 5, and 25 mg/kg
Administration: Injected s.c.; twice a day
Result: Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels.
Animal Model: Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf[1]
Dosage: 10 and 50 mg/kg
Administration: Administered orally; twice a day for 6 weeks
Result: Partly prevented bone loss.

分子量

443.54

Formula

C26H29N5O2
CAS 号

234772-64-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

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

  • [1]. Missbach M, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellularsubstrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.

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

(S)-3-Hydroxy Midostaurin(Synonyms: (S)-CGP52421)

发表于由

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。

(S)-3-Hydroxy Midostaurin (Synonyms: (S)-CGP52421)

(S)-3-Hydroxy Midostaurin ((S)-CGP52421) 是一种有效的激酶抑制剂，对 VEGFR-2，TRK-A，FLT3 等 13 种激酶的 IC50 值为 <400 nM。(S)-3-Hydroxy Midostaurin 是 Midostaurin (PKC412; HY-10230) 通过肝 CYP3A4 酶代谢的次要代谢产物。(S)-3-Hydroxy Midostaurin 具有潜在的用于急性髓细胞性白血病 (AML) 的潜力。

(S)-3-Hydroxy Midostaurin(Synonyms: (S)-CGP52421)

(S)-3-Hydroxy Midostaurin Chemical Structure

CAS No. : 945260-14-0

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

(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nm for 13 kinases (vegfr-2, trk-a, flt3, et). (s)-3-hydroxy midostaurin is a minor metabolite of (pkc412; hy-10230) undergoing by the hepatic cyp3a4 enzyme. has potential acute myeloid leukemia (aml)[1].

体外研究
(In Vitro)

(S)-3-Hydroxy Midostaurin ((S)-CGP52421; compound 4) has IC50 values in the range of 200-400 nM against the ITD and D835Y mutants and low micromolar activity against the wild-type enzyme[1].
The epimeric mixture of metabolites ((R)-3-Hydroxy Midostaurin + (S)-3-Hydroxy Midostaurin) substantially inhibits the proliferation of only the Tel-PDGFRβ (GI50=63 nM), KIT D816V (GI50=320 nM), and FLT3-ITD (GI50=650 nM) BaF3 cell lines, while the wild-type cells are relatively insensitive[1].

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

586.64

Formula

C35H30N4O5
CAS 号

945260-14-0
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]. Manley PW, et al. Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its PredominantMetabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy. Biochemistry. 2018 Sep 25;57(38):5576-5590.

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

(R)-3-Hydroxy Midostaurin(Synonyms: (R)-CGP52421)

发表于由

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。

(R)-3-Hydroxy Midostaurin (Synonyms: (R)-CGP52421)

(R)-3-Hydroxy Midostaurin ((R)-CGP52421) 是有效的激酶抑制剂。(R)-3-Hydroxy Midostaurin 是 Midostaurin (PKC412; HY-10230) 通过肝 CYP3A4 酶代谢的主要代谢产物。(R)-3-Hydroxy Midostaurin 具有潜在的用于急性髓细胞性白血病 (AML) 的潜力。

(R)-3-Hydroxy Midostaurin(Synonyms: (R)-CGP52421)

(R)-3-Hydroxy Midostaurin Chemical Structure

CAS No. : 155848-20-7

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

(R)-3-Hydroxy Midostaurin ((R)-CGP52421) is a potent kinases inhibitor. (R)-3-Hydroxy Midostaurin is a major metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (R)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML)[1].

体外研究
(In Vitro)

(R)-3-Hydroxy Midostaurin ((R)-CGP52421; compound 5) has IC50 values in the range of 200-400 nM against the ITD and D835Y mutants and low micromolar activity against the wild-type enzyme[1].
The epimeric mixture of metabolites ((R)-3-Hydroxy Midostaurin + (S)-3-Hydroxy Midostaurin) substantially inhibits the proliferation of only the Tel-PDGFRβ (GI50=63 nM), KIT D816V (GI50=320 nM), and FLT3-ITD (GI50=650 nM) BaF3 cell lines, while the wild-type cells are relatively insensitive[1].

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

586.64

Formula

C35H30N4O5
CAS 号

155848-20-7
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]. Manley PW, et al. Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its PredominantMetabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy. Biochemistry. 2018 Sep 25;57(38):5576-5590.

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

(S)-3-Hydroxy Midostaurin(Synonyms: (S)-CGP52421)

发表于由

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。

(S)-3-Hydroxy Midostaurin (Synonyms: (S)-CGP52421)

(S)-3-Hydroxy Midostaurin ((S)-CGP52421) 是一种有效的激酶抑制剂，对 VEGFR-2，TRK-A，FLT3 等 13 种激酶的 IC50 值为 <400 nM。(S)-3-Hydroxy Midostaurin 是 Midostaurin (PKC412; HY-10230) 通过肝 CYP3A4 酶代谢的次要代谢产物。(S)-3-Hydroxy Midostaurin 具有潜在的用于急性髓细胞性白血病 (AML) 的潜力。

(S)-3-Hydroxy Midostaurin(Synonyms: (S)-CGP52421)

(S)-3-Hydroxy Midostaurin Chemical Structure

CAS No. : 945260-14-0

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

(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nm for 13 kinases (vegfr-2, trk-a, flt3, et). (s)-3-hydroxy midostaurin is a minor metabolite of (pkc412; hy-10230) undergoing by the hepatic cyp3a4 enzyme. has potential acute myeloid leukemia (aml)[1].

体外研究
(In Vitro)

(S)-3-Hydroxy Midostaurin ((S)-CGP52421; compound 4) has IC50 values in the range of 200-400 nM against the ITD and D835Y mutants and low micromolar activity against the wild-type enzyme[1].
The epimeric mixture of metabolites ((R)-3-Hydroxy Midostaurin + (S)-3-Hydroxy Midostaurin) substantially inhibits the proliferation of only the Tel-PDGFRβ (GI50=63 nM), KIT D816V (GI50=320 nM), and FLT3-ITD (GI50=650 nM) BaF3 cell lines, while the wild-type cells are relatively insensitive[1].

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

586.64

Formula

C35H30N4O5
CAS 号

945260-14-0
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]. Manley PW, et al. Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its PredominantMetabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy. Biochemistry. 2018 Sep 25;57(38):5576-5590.

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

(R)-3-Hydroxy Midostaurin(Synonyms: (R)-CGP52421)

发表于由

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。

(R)-3-Hydroxy Midostaurin (Synonyms: (R)-CGP52421)

(R)-3-Hydroxy Midostaurin ((R)-CGP52421) 是有效的激酶抑制剂。(R)-3-Hydroxy Midostaurin 是 Midostaurin (PKC412; HY-10230) 通过肝 CYP3A4 酶代谢的主要代谢产物。(R)-3-Hydroxy Midostaurin 具有潜在的用于急性髓细胞性白血病 (AML) 的潜力。

(R)-3-Hydroxy Midostaurin(Synonyms: (R)-CGP52421)

(R)-3-Hydroxy Midostaurin Chemical Structure

CAS No. : 155848-20-7

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

(R)-3-Hydroxy Midostaurin ((R)-CGP52421) is a potent kinases inhibitor. (R)-3-Hydroxy Midostaurin is a major metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (R)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML)[1].

体外研究
(In Vitro)

(R)-3-Hydroxy Midostaurin ((R)-CGP52421; compound 5) has IC50 values in the range of 200-400 nM against the ITD and D835Y mutants and low micromolar activity against the wild-type enzyme[1].
The epimeric mixture of metabolites ((R)-3-Hydroxy Midostaurin + (S)-3-Hydroxy Midostaurin) substantially inhibits the proliferation of only the Tel-PDGFRβ (GI50=63 nM), KIT D816V (GI50=320 nM), and FLT3-ITD (GI50=650 nM) BaF3 cell lines, while the wild-type cells are relatively insensitive[1].

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

586.64

Formula

C35H30N4O5
CAS 号

155848-20-7
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]. Manley PW, et al. Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its PredominantMetabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy. Biochemistry. 2018 Sep 25;57(38):5576-5590.

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

PCR板硅胶片,于96孔PCR板,“-”开口,白色CGP-9-W-

发表于由

PCR板硅胶片,于96孔PCR板,“-”开口,白色

  • 产品型号：CGP-9-W-
  • 简要描述：PCR板硅胶片,于96孔PCR板,“-“开口,白色上海金畔生物科技有限公司供应：光度计，检测仪，免疫仪，全系荧光定量PCR耗材，移液器，钻石吸嘴，离心管，冻存管，培养皿，培养板，培养瓶，吸头，仪器及手套，色谱耗材，针头过滤器。
产品咨询在线客服
  • 产品简介

PCR板硅胶片,于96孔PCR板,“-”开口,白色上海金畔生物科技有限公司供应：光度计，检测仪，移液器，钻石吸嘴，离心管，冻存管，培养皿，全系荧光定量PCR耗材。

PCR 板      

CG编号   ：CGP-9-W-

产品描述  ：PCR板硅胶片，适用于96孔PCR板，“-”开口，白色

包装规格  ： 10片/袋，5袋/箱(50片/箱）

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CGP-9-WS-    PCR板硅胶片，适用于96孔PCR板，“-”开口，白色，灭菌    10片/袋，5袋/箱(50片/箱）    

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23-2085    0.5mlPCR单管，薄壁，透明，平盖，非灭菌    1000支/包，10包/箱（10000支/箱）    
进口PCR            
L-2081    0.2ml 8联排超薄清晰PCR管, 无DNA酶无RNA酶无热源, 无色.       125 条/包, 10包/箱    
L-2082    0.2ml 8联排管盖, 拱顶盖(凸盖), 无DNA酶无RNA酶无热源, 无色.      125 条/包 10盒/箱 (包装在L-2081 箱内)    
L-2087    0.2ml 8联排实时荧光定量PCR管,  超薄壁 无DNA酶无RNA酶无热源, 无色.     125 条/盒, 10盒/箱     
L-2088    0.2ml 8联排实时荧光定量PCR管盖, 平盖, 无DNA酶无RNA酶无热源, 无色.     125条/包，10包/箱 (包装在L-2087 箱内)    
PCR板            
23-2197N    200μl 96孔无裙边 PCR 板，透明，非灭菌    10块/袋，5袋/箱(50块/箱）    
23-35601    200μl 96孔半裙边 PCR 板，透明，非灭菌    10块/袋，5袋/箱(50块/箱）    
23-35601B    200μl 96孔半裙边 PCR 板，黑色，非灭菌    10块/袋，5袋/箱(50块/箱）    适应客户：医院检验科PCR实验室，中心实验室，肝病中心；第三方检测机构，科研院所，大专院校，制药厂，试剂生产厂家，疾控中心，检验检疫。 

 

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