Samuraciclib (ICEC0942, CT7001) is a novel oral CDK7 inhibitor with an IC50 of 40 nM. It has IC50 values for other CDK proteins such as CDK1, CDK2, CDK5 and CDK9 as 45, 15, 230 and 30 times higher than that of CDK7 IC50, respectively. ICEC0942 (CT7001) promotes cell cycle blocking and apoptosis.
Molecular Weight | 430.98 |
Formula | C22H31ClN6O |
CAS Number | 1805789-54-1 |
Solubility (25°C) | DMSO ≥ 60 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] No authors listed. Carteolol
[4] S HIFT, et al. Wien Med Wochenschr. [Prothipendyl-hydrochloride, a new neuroleptic]
[5] S Groszkowski, et al. Pol J Pharmacol Pharm. 1-Haloacylpiperazines
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