Pemigatinib (INCB054828) is an orally effective, selective FGFR inhibitor with IC50 values of 0.4 nM, 0.5 nM, 1.2 nM, and 30 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.Pemigatinib binds to and inhibits FGFR1/2/3, which inhibits proliferation in FGFR1/2/3 overexpressing tumor cells. pemigatinib exhibited antitumor activity in mouse xenograft models of human tumors with altered FGFR1, FGFR2 or FGFR3.
Molecular Weight | 487.5 |
Formula | C24H27F2N5O4 |
CAS Number | 1513857-77-6 |
Solubility (25°C) | DMSO ≥ 32 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.
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