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Chemical Structure : Rogaratinib
CAS No.: 1443530-05-9
Catalog No.: 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 | $378 | In stock | |
| 10 mg | $558 | In stock | |
| 25 mg | $958 | In stock | |
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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.
| M.Wt | 466.56 | |
| Formula | C23H26N6O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO (Ultrasonic needed) |
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| 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 |
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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.
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