-CR8 trihydrochloride.gif)
(R)-CR8 trihydrochloride, one of the isomers of CR8, is a potent CDK1/2/5/7/9 inhibitor with anti-proliferative and pro-apoptotic effects on CML cell lines. (R)-CR8 trihydrochloride inhibited CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM ), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM).
| Molecular Weight | 468 |
| Formula | C24H30ClN7O |
| CAS Number | 1786438-30-9 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage | 2-8°C, dry, sealed |
| 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.
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