Rogaratinib |CAS:1443530-05-9 Probechem Biochemicals

Chemical Structure : Rogaratinib

CAS No.: 1443530-05-9

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Rogaratinib (BAY 1163877, BAY1163877)

货号: PC-61963Not For Human Use, Lab Use Only.

Rogaratinib (BAY 1163877) is a potent, selective, orally available pan-FGFR with IC50 of 15, <1, 19 and 33 nM for FGFR1, 2, 3 and 4, respectively.

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5 mg	￥3780	In stock
10 mg	￥5580	In stock
25 mg	￥9580	In stock
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100 mg		Get quote

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生物&药学活性

Rogaratinib (BAY 1163877) is a potent, selective, orally available pan-FGFR with IC50 of 15, <1, 19 and 33 nM for FGFR1, 2, 3 and 4, respectively.
BAY 1163877 weakly inhibits VEGFR2 with IC50 of 120 nM, exhibits Ki of 1.6, 5.0, 7.8 and 7.6 nM for FGFR1, 2, 3 and 4 in competition binding assay, no significant affitnity for VEGFR2 (19% inhibition at 100 nM).
BAY 1163877 inhibits FGFb-stimulated HUVEC proliferation with IC50 of 16 nM, 28-fold selectivity over VEGF-stimulated.
BAY 1163877 demonstrates tumor growth reduction in pre-clinical models bearing different FGFR alterations both in mono- and combination therapy.

物理化学性质&存储条件

分子量	466.56
分子式	C23H26N6O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO (Ultrasonic needed)
Chemical Name/SMILES	4-((4-amino-5-(7-methoxy-5-methylbenzo[b]thiophen-2-yl)-6-(methoxymethyl)pyrrolo[2,1-f][1,2,4]triazin-7-yl)methyl)piperazin-2-one

参考文献

1. Kim SM, et al. Oncogenesis. 2016 Jul 18;5(7):e241.

2. Collin MP, et al. ChemMedChem. 2018 Feb 16. doi: 10.1002/cmdc.201700718.

Rogaratinib (BAY 1163877, BAY1163877)

生物&药学活性

物理化学性质&存储条件

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Rogaratinib (BAY 1163877, BAY1163877)

生物&药学活性

物理化学性质&存储条件

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