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Samuraciclib hydrochloride hydrate
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议

半岛bd体育手机客户端 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。
别名CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
分子式C22H30N6O.(2.5HCl).(2H2O)
分子量521.7
溶解度DMSO : 100 mg/mL (191.68 mM; Need ultrasonic)
储存条件4°C, stored under nitrogen, away from moisture
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

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[1][2].

Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment promotes cell apoptosis[1].Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment induces cell cycle arrest[1].Samuraciclib hydrochloride hydrate (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 trihydrochloride also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma[1].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[1].

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[1].The combination of Samuraciclib (ICEC0942) hydrochloride hydrate and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts[1].

[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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