Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 4-[[5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]-2-pyrimidinyl]amino]-1H-pyrazole-1-ethanol
Purity: ≥98%
Formula Markup: C18H19F2N5O4
Formula Weight: 407.4
CAS Number: 1453208-66-6
Notes: ASP5878 is an inhibitor of wild-type FGFR1, -2, -3, and -4 (IC50s = 0.47, 0.6, 0.74, and 3.5 nM, respectively) and mutant FGFR3K650E, FGFR3K560M, and FGFR4N535K (IC50s = 1.6, 4.2, and 78 nM, respectively).{51916} It is selective for these FGFRs over a panel of 128 additional kinases at 200 nM but does inhibit VEGFR2 and CSF-1 receptor tyrosine kinase (FMS; IC50s = 25 and 150 nM, respectively). It selectively inhibits the proliferation of urothelial cancer cell lines with FGFR gene alterations (IC50s = FGFR gene alterations (IC50s = ≥300 nM). ASP5878 also inhibits the proliferation of adriamycin-resistant UM-UC-14 bladder cancer cells and gemcitabine-resistant RT-112 bladder cancer cells (IC50s = 11 and 10 nM, respectively). In vivo, ASP5878 (3 mg/kg) induces tumor regression in a UM-UC-14 mouse xenograft model. It also increases femur and tibia length and femur growth plate cartilage thickness in Fgfr3G380R male mice in a model of achondroplasia when administered at a dose of 300 µg/kg.{51917}
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