Samuraciclib(Synonyms: CT7001; ICEC0942)

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。

Samuraciclib (Synonyms: CT7001; ICEC0942)

Samuraciclib (CT7001) 是一种有效的,具有选择性,ATP 竞争性和口服活性的 CDK7 抑制剂,IC50 为 41 nM。Samuraciclib 对 CDK7 的选择性分别是 CDK1,CDK2 (IC50 为 578 nM),CDK5 和 CDK9 的 45 倍,15 倍,230 倍和 30 倍。Samuraciclib 以 GI50 值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长,具有有效的抗肿瘤作用。

Samuraciclib(Synonyms: CT7001;  ICEC0942)

Samuraciclib Chemical Structure

CAS No. : 1805833-75-3

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Samuraciclib 的其他形式现货产品:

Samuraciclib hydrochloride Samuraciclib hydrochloride hydrate

生物活性

Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib has anti-tumor effects[1][2].

IC50 & Target[1][2]

CDK7/CycH/MAT1

41 nM (IC50)

CDK2/cycE1

578 nM (IC50)

CDK1

1.8 μM (IC50)

CDK4

49 μM (IC50)

CDK5

9.4 μM (IC50)

CDK6

34 μM (IC50)

CDK9

1.2 μM (IC50)

体外研究
(In Vitro)

Samuraciclib (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment promotes cell apoptosis[1].
Samuraciclib (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment induces cell cycle arrest[1].
Samuraciclib (ICEC0942; 0-10 µM; 0-24 hours; HCT116 cells) treatment inhibits the phosphorylation of PolII CTD in a dose and time dependent manner in HCT116 colon cancer cells. Samuraciclib also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma[1].
Samuraciclib (ICEC0942) inhibits the growth of MCF7, T47D, MDA-MB-231, HS578T, MDA-MB-468, MCF10A and HMEC cells with GI50 values of 0.18 µM, 0.32 µM, 0. 33 µM, 0.21 µM, 0.22 µM, 0.67 µM and 1.25 µM, respectively[1].

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

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0 µM, 0.1 µM, 1 µM and 10 µM
Incubation Time: 24 hours
Result: Induced caspase 3/7 and demonstrated PARP cleavage.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 0 µM, 0.01 µM, 0.1 µM, 1 µM and 10 µM
Incubation Time: 24 hours
Result: Showed accumulation of cells in G2/M.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0 µM, 0.1 µM, 1 µM and 10 µM
Incubation Time: 0 hour, 4 hours, 8 hours, 16 hours or 24 hours
Result: PolII CTD phosphorylation was inhibited in a dose and time dependent manner in HCT116 colon cancer cells.

体内研究
(In Vivo)

Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days; female nu/nu-BALB/c athymic nude mice) treatment inhibits tumor growth by 60% at day 14, and is accompanied by highly significant reductions in PolII Ser2 and Ser5 phosphorylation in PBMCs and in tumors[1].
The combination of Samuraciclib (ICEC0942) and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts[1].

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

Animal Model: Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells[1].
Dosage: 100 mg/kg
Administration: Oral gavage; daily; for 14 days
Result: At day 14, tumor growth was inhibited by 60%.

分子量

394.51

Formula

C22H30N6O

CAS 号

1805833-75-3

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.

参考文献
  • [1]. Patel H, et al. ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment. Mol Cancer Ther. 2018 Jun;17(6):1156-1166.

    [2]. Hazel P, et al. Inhibitor Selectivity for Cyclin-Dependent Kinase 7: A Structural, Thermodynamic, and Modelling Study. ChemMedChem. 2017 Mar 7;12(5):372-380.

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