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  • 化合物 Samuraciclib|T61835|TargetMol

化合物 Samuraciclib|T61835|TargetMol

Samuraciclib
1805833-75-3
17500 100mg 起订
13800 50mg 起订
10600 25mg 起订
上海 更新日期:2024-12-12

TargetMol中国(陶术生物)

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联系人:邵小姐
手机:4008200310 拨打
邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 Samuraciclib
英文名称:
Samuraciclib
CAS号:
1805833-75-3
品牌:
TargetMol
产地:
美国
保存条件:
Shipping with blue ice.
产品类别:
抑制剂
货号:
T61835

Product Introduction

Bioactivity

名称Samuraciclib
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%.
存储条件Shipping with blue ice.
Samuraciclib|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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