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Pemigatinib

Cat. No. M9596
Pemigatinib Structure
Synonym:

INCB054828

Size Price Availability Quantity
2mg USD 90  USD90 In stock
5mg USD 120  USD120 In stock
10mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
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. Pharmacol Res. The Role of Fibroblast Growth Factor Receptor (FGFR) Protein-Tyrosine Kinase Inhibitors in the Treatment of Cancers Including Those of the Urinary Bladder

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Keywords: Pemigatinib, INCB054828 supplier, FGFR, inhibitors, activators


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