Basic information Safety Supplier Related

BAY-1163877

Basic information Safety Supplier Related

BAY-1163877 Basic information

Product Name:
BAY-1163877
Synonyms:
  • BAY-1163877
  • Rogaratinib
  • 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
  • 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]-
  • Rogaratinib,inhibit,BAY 1163877,Fibroblast growth factor receptor,BAY-1163877,FGFR,Inhibitor
CAS:
1443530-05-9
MF:
C23H26N6O3S
MW:
466.56
Mol File:
1443530-05-9.mol
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BAY-1163877 Chemical Properties

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
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BAY-1163877 Usage And Synthesis

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

BAY-1163877Supplier

Shanghai Topbiochem Technology Co., Ltd
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