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Samuraciclib hydrochloride (ICEC0942 hydrochloride) 是一种具有选择性,ATP 竞争性和口服活性的CDK7抑制剂,IC50为 41 nM。它以 GI50值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长,具有抗肿瘤作用。
Samuraciclib hydrochloride (ICEC0942 hydrochloride) 是一种具有选择性,ATP 竞争性和口服活性的CDK7抑制剂,IC50为 41 nM。它以 GI50值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长,具有抗肿瘤作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 817 | 现货 | |
2 mg | ¥ 1,100 | 现货 | |
5 mg | ¥ 1,980 | 现货 | |
10 mg | ¥ 3,390 | 现货 | |
25 mg | ¥ 5,280 | 现货 | |
50 mg | ¥ 7,450 | 现货 | |
100 mg | ¥ 9,850 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 2,210 | 现货 |
产品描述 | Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects. |
靶点活性 | CDK1-CyclinA:1.8 μM, CDK5-p35 NCK:9.4 μM, CDK2-CyclinA:578 nM, CDK7-CyclinH:41 nM, CDK9-CyclinT1:1.2 μM, CDK4-CyclinD1:49 μM, CDK6-CyclinD1:34 μM |
体外活性 | Samuraciclib(ICEC0942;0-10 μM;24小时;HCT116细胞)处理能促进细胞凋亡,并引起细胞周期阻滞。该化合物在剂量和时间依赖性方式内抑制HCT116结肠癌细胞中PolII CTD的磷酸化,并阻断CDK1、CDK2以及视网膜母细胞瘤蛋白的磷酸化。Samuraciclib(ICEC0942)对MCF7、T47D、MDA-MB-231、HS578T、MDA-MB-468、MCF10A及HMEC细胞的生长抑制具有GI50值分别为0.18 μM、0.32 μM、0.33 μM、0.21 μM、0.22 μM、0.67 μM及1.25 μM。 |
体内活性 | Samuraciclib(ICEC0942;100 mg/kg;口服管饲;每日一次;连续14天;雌性nu/nu-BALB/c无胸腺裸鼠)治疗在第14天抑制60%的肿瘤体积增长,抑制外周血单核细胞(PBMC)及肿瘤中PolII Ser2和Ser5的磷酸化。Samuraciclib(ICEC0942)与ICI 47699联合治疗显示了雌激素受体(ER)阳性肿瘤异种移植物的完全停滞。 |
别名 | ICEC0942 hydrochloride, CT7001 hydrochloride |
分子量 | 430.97 |
分子式 | C22H31ClN6O |
CAS No. | 1805789-54-1 |
Smiles | Cl.CC(C)c1cnn2c(NCc3ccccc3)cc(NC[C@H]3CCNC[C@@H]3O)nc12 |
密度 | no data available |
存储 | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 55 mg/mL (127.62 mM), Sonication is recommended. DMSO: 25 mg/mL (58.01 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
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