| Identification | Back Directory | [Name]
BAY-1163877 | [CAS]
1443530-05-9 | [Synonyms]
BAY-1163877
Rogaratinib
Rogaratinib (BAY1163877)
2-Piperazinone, 4-[[4-amino-6-(methoxymethyl)-5-(7-methoxy-5-methylbenzo[b]thien-2-yl)pyrrolo[2,1-f][1,2,4]triazin-7-yl]methyl]-
4-{[4-amino-6-(methoxymethyl)-5-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrrolo[2,1-f]-[1,2,4]triazin-7-yl]methyl}piperazin-2-one | [Molecular Formula]
C23H26N6O3S | [MOL File]
1443530-05-9.mol | [Molecular Weight]
466.56 |
| Chemical Properties | Back Directory | [density ]
1.48±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:5.0(Max Conc. mg/mL);10.72(Max Conc. mM) | [form ]
Solid | [pka]
15.49±0.20(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
Rogaratinib (BAY1163877) is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor. Rogaratinib inhibits FGFRs with IC50s of 11.2 nM (FGFR1), <1 nM (FGFR2), 18.5 nM (FGFR3), 127 nM (VEGFR3/FLT4), 201 nM (FGFR4), respectively[1][2]. | [IC 50]
FGFR1; FGFR2; FGFR3; FGFR4 | [References]
[1] Heroult M, et al. Preclinical profile of BAY 1163877-a selective pan-FGFR inhibitor in phase 1 clinical trial[J]. Cancer Res, 2014, 74(suppl 19): 1739a.
[2] Kim SM, et al. Activation of the Met kinase confers acquired drug resistance in FGFR-targeted lung cancer therapy. Oncogenesis. 2016 Jul 18;5(7):e241. DOI:10.1038/oncsis.2016.48 |
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