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PRN1371

Cat. No. M10737
PRN1371  Structure
Size Price Availability Quantity
5mg USD 300  USD300 In stock
10mg USD 500  USD500 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PRN1371 is a highly selective and potent inhibitor of FGFR1-4 and CSF1R against FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R IC50 The values are 0.6, 1.3, 4.1, 19.3, and 8.1 nM, respectively.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 561.46
Formula C26H30Cl2N6O4
CAS Number 1802929-43-6
Purity >99%
Solubility DMSO ≥ 20 mg/mL
Storage at -20°C
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

[2] M -L Nairismgi, et al. Leukemia. Oncogenic activation of JAK3-STAT signaling confers clinical sensitivity to PRN371, a novel selective and potent JAK3 inhibitor, in natural killer/T-cell lymphoma

[3] Eleni Venetsanakos, et al. Mol Cancer Ther. The Irreversible Covalent Fibroblast Growth Factor Receptor Inhibitor PRN1371 Exhibits Sustained Inhibition of FGFR after Drug Clearance

[4] Ken A Brameld, et al. J Med Chem. Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors

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  Catalog
Abmole Inhibitor Catalog




Keywords: PRN1371 supplier, FGFR, inhibitors

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