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Pemigatinib (INCB054828) is an orally bioavailable inhibitor of FGFR with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib binds to and inhibits FGFR1/2/3, which may result in the inhibition of FGFR1/2/3-related signal transduction pathways.
| 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.
| Molecular Weight | 487.5 |
| Formula | C24H27F2N5O4 |
| CAS Number | 1513857-77-6 |
| Purity | 99.79% |
| Solubility | DMSO ≥ 32 mg/mL |
| Storage | at -20°C |
| Related FGFR Products |
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EOC317 (ACTB-1003) is an orally available kinase inhibitor that inhibits FGFR1, VEGFR2, and tie-2 with IC50 values of 6,2, and 4 nM, respectively. |
| PRN1371
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| Alofanib (RPT835)
Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells. |
| ASP5878
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PF-05231023 is an FGF21-receptor agonist, it is also a potential treatment for T2DM. |
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