PF-06873600 is an orally bioavailable, cyclin-dependent kinase (CDK) inhibitor, with potential antineoplastic activity. PF-06873600 has Ki values of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. PF-06873600 selectively targets, binds to and inhibits the activity of CDKs. Inhibition of these kinases leads to cell cycle arrest, induction of apoptosis and inhibition of tumor cell proliferation.
| Molecular Weight | 471.52 |
| Formula | C20H27F2N5O4S |
| CAS Number | 2185857-97-8 |
| Solubility (25°C) | DMSO ≥ 50 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.
[1] Kevin Freeman-Cook, et al. Expanding control of the tumor cell cycle with a CDK2/4/6 inhibitor
[2] Rinath Jeselsohn, et al. Restoring order at the cell cycle border: Co-targeting CDK4/6 and CDK2
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