Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)-8-[3-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]propyl]-pyrido[2,3-d]pyrimidin-7(8H)-one
Purity: ≥98%
Formula Markup: C26H30Cl2N6O4
Formula Weight: 561.45984
CAS Number: 1802929-43-6
Notes: PRN-1371 is an irreversible covalent pan-FGFR inhibitor (IC50s = 0.7, 1.3, 4.4, and 19.3 nM for FGFR-1, -2, -3, and -4, respectively).{54899} It is selective for FGFR over VEGFR2 (IC50 = 705 nM) and a panel of 250 kinases (IC50s = >1 µM for all) but does inhibit colony stimulating factor 1 receptor (CSF1R) activity by greater than 90% at 1 µM. PRN-1371 inhibits proliferation in a panel of ten cancer cell lines containing various FGFR mutants (IC50s = 2-231 nM) and induces apoptosis in SNU-16 gastric and RT4 bladder cancer cells (EC50s = 15.9 and 11.8 nM, respectively). It reduces tumor growth in an SNU-16 mouse xenograft model and a patient-derived xenograft (PDX) mouse model of liver cancer when administered at a dose of 15 mg/kg twice per day.
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