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 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
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Samuraciclib hydrochloride hydrate
CAS number：unknown molecular formula：C22H33ClN6O2
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| Chinese alias | 萨莫拉西利盐酸盐水合物 | ||
| English alias | - | ||
| CAS number | unknown | molecular formula | C22H33ClN6O2 |
| molecular weight | 552.33 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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