Samuraciclib hydrochloride hydrate

萨莫拉西利盐酸盐水合物

Samuraciclib hydrochloride hydrate

S659091-5mg

5mg

≥99%

2-8°C储存,充氩,干燥

冰袋运输

Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC 50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1 , CDK2 (IC 50 of 578 Appearance:Solid IC50& Target:CDK7/CycH/MAT1|41 nM (IC|50|)|CDK2/cycE1|578 nM (IC|50|)|CDK1|1.8 μM (IC|50|)|CDK4|49 μM (IC|50|)|CDK5|9.4 μM (IC|50|)|CDK6|34 μM (IC|50|)|CDK9|1.2 μM (IC|50|) In Vitro: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 (I In Vivo:Samuraciclib (ICEC0942; 100mg/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 p Biological Activity:Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC 50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1 , CDK2 (IC 50 of 578

C22H30N6O.(2.5HCl).(2H2O)

521.7 g/mol

O[C@H]1CNCC[C@@H]1CNC2=NC3=C(C(C)C)C=NN3C(NCC4=CC=CC=C4)=C2.Cl.O.O.[2.5]

DMSO : 100 mg/mL (191.68 mM; Need ultrasonic)

包含CDK，MAPK，GSK3，CLK家族