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Samuraciclib

产品编号 T61835 CAS 1805833-75-3

Samuraciclib (CT7001) is a potent, selective, and orally active inhibitor of CDK7, with an ATP-competitive nature. It effectively inhibits CDK7 with an IC 50 value of 41 nM. Furthermore, Samuraciclib demonstrates remarkable selectivity ratios, with 45-fold, 15-fold, 230-fold, and 30-fold selectivity over CDK1, CDK2 (IC 50 of 578 nM), CDK5, and CDK9, respectively. Notably, Samuraciclib has been found to inhibit the growth of breast cancer cell lines, exhibiting GI 50 values ranging between 0.2-0.3 μM. Additionally, Samuraciclib has been observed to possess anti-tumor effects [1] [2]. 在相同实验条件下，摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性，但盐形式 Samuraciclib hydrochloride 的水溶性和稳定性通常比游离态更好。

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Samuraciclib, CAS 1805833-75-3

规格	价格/CNY	货期
25 mg	￥ 10,600	10-14周
50 mg	￥ 13,800	10-14周
100 mg	￥ 17,500	10-14周

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Samuraciclib 的其他形式现货产品:

Samuraciclib hydrochloride

其他形式的 Samuraciclib:

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生物活性

化学信息

存储 & 溶解度

产品描述	Samuraciclib (CT7001) is a potent, selective, and orally active inhibitor of CDK7, with an ATP-competitive nature. It effectively inhibits CDK7 with an IC 50 value of 41 nM. Furthermore, Samuraciclib demonstrates remarkable selectivity ratios, with 45-fold, 15-fold, 230-fold, and 30-fold selectivity over CDK1, CDK2 (IC 50 of 578 nM), CDK5, and CDK9, respectively. Notably, Samuraciclib has been found to inhibit the growth of breast cancer cell lines, exhibiting GI 50 values ranging between 0.2-0.3 μM. Additionally, Samuraciclib has been observed to possess anti-tumor effects [1] [2].
体外活性	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 GI 50 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]. 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.
体内活性	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]. 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
分子式	C22H30N6O
CAS No.	1805833-75-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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