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H3B-6527

Cat. No. M5242
H3B-6527 Structure
Size Price Availability Quantity
5mg USD 230  USD230 In stock
10mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

H3B-6527 (H3 Biomedicine) is a highly selective FGFR4 inhibitor with potent antitumour activity in FGF19 amplified cell lines and mice.

Chemical Information
Molecular Weight 629.54
Formula C29H34Cl2N8O4
CAS Number 1702259-66-2
Solubility (25°C) ≥ 6.3 mg/mL in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Robert Roskoski Jr. The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder

[2] F Colombo, et al. Correlation of the in vitro biotransformation of H3B-6527 in dog and human hepatocytes with the in vivo metabolic profile of 14 C-H3B-6527 in a dog mass balance study

[3] Liwei Lang, et al. Fibroblast Growth Factor Receptor 4 Targeting in Cancer: New Insights into Mechanisms and Therapeutic Strategies

[4] Nathalie Rioux, et al. Effect of a high-fat meal on the relative bioavailability of H3B-6527, a novel FGFR4 inhibitor, in healthy volunteers

[5] Jaya Julie Joshi, et al. H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma

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