Samuraciclib hydrochloride hydrate CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate|西域试剂

Samuraciclib hydrochloride hydrate CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate,99.88%

产品编号：Bellancom-103712C| 分子式：C₂₂H₃₃ClN₆O₂| 分子量：552.33

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-103712C	￥2500.00	杭州北京（现货）
Bellancom-103712C	￥4200.00	杭州北京（现货）
Bellancom-103712C	￥8600.00	杭州北京（现货）
Bellancom-103712C	￥14000.00	杭州北京（现货）

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Samuraciclib hydrochloride hydrate CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate

产品介绍

Samuraciclib (CT7001) hydrochloride hydrate 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 hydrochloride hydrate 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 hydrochloride hydrate 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。

生物活性

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

体外研究

Samuraciclib (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) hydrochloride hydrate treatment promotes cell apoptosis.
Samuraciclib (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) hydrochloride hydrate treatment induces cell cycle arrest.
Samuraciclib (ICEC0942; 0-10 µM; 0-24 hours; HCT116 cells) hydrochloride hydrate treatment inhibits the phosphorylation of PolII CTD in a dose and time dependent manner in HCT116 colon cancer cells. Samuraciclib hydrochloride hydrate also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma.
Samuraciclib (ICEC0942) hydrochloride hydrate 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

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

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

Western Blot Analysis

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) hydrochloride hydrate 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.
The combination of Samuraciclib (ICEC0942) and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts.

西域 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.
Dosage:	100 mg/kg
Administration:	Oral gavage; daily; for 14 days
Result:	At day 14, tumor growth was inhibited by 60%.

体内研究

西域 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.
Dosage:	100 mg/kg
Administration:	Oral gavage; daily; for 14 days
Result:	At day 14, tumor growth was inhibited by 60%.

体内研究

西域 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.
Dosage:	100 mg/kg
Administration:	Oral gavage; daily; for 14 days
Result:	At day 14, tumor growth was inhibited by 60%.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (181.05 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8105 mL	9.0526 mL	18.1051 mL
5 mM	0.3621 mL	1.8105 mL	3.6210 mL
10 mM	0.1811 mL	0.9053 mL	1.8105 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。

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)

参考文献