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H3B-6527 (H3 Biomedicine) is a highly selective FGFR4 inhibitor with potent antitumour activity in FGF19 amplified cell lines and mice.
| 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 | 629.54 |
| Formula | C29H34Cl2N8O4 |
| CAS Number | 1702259-66-2 |
| Purity | 99.13% |
| Solubility | ≥ 6.3 mg/mL in DMSO |
| 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
PF-05231023 is an FGF21-receptor agonist, it is also a potential treatment for T2DM. |
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