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Rogaratinib

Chemical Structure : Rogaratinib

CAS No.: 1443530-05-9

Rogaratinib (BAY 1163877, BAY1163877)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 466.56
Formula C23H26N6O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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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