Chemical Structure : ISM7594
CAS No.:
3025799-76-9
ISM7594
(ISM-7594)
Catalog No.: PC-24856Not For Human Use, Lab Use Only.
ISM7594 is a potent, selective and covalent FGFR2/3 inhibitor with IC50 of 1.4/12.7 nM respectively, inhibits FGFR2 mutants and FGFR3 mutants with IC50 of 0.22-5.9 nM and 3.7-26 nM, selectively spares FGFR1/4.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
ISM7594 is a potent, selective and covalent FGFR2/3 inhibitor with IC50 of 1.4/12.7 nM respectively, inhibits FGFR2 mutants and FGFR3 mutants with IC50 of 0.22-5.9 nM and 3.7-26 nM, selectively spares FGFR1/4.
ISM7594 exhibits robust suppression of both p-FGFR2 and p-ERK, with IC50 values of 1.5 and 2.1 nM, respectively, in SNU-16 cell line, exhibits antiproliferative IC50 of 1.6 nM.
ISM7594 demonstrates dual antiproliferation with average IC50 values of 4.5 and 7.3 nM against FGFR2- and FGFR3-altered cancer cells, respectively.
ISM7594 (30-60 mpk, BID) exhibits antitumor efficacy in 21-day SNU-16/RT4 xenograft models in Balb/c nude mice.
Physicochemical Properties
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M.Wt
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540.53
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Formula
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C29H22F2N6O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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6-(3-Fluoro-4-((4-methylpyrimidin-2-yl)oxy)phenyl)-7-(4-(2-fluoroacrylamido)phenyl)-3-methylpyrrolo[1,2-b]pyridazine-5-carboxamide
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References
1. Yazhou Wang, et al. J Med Chem. 2025 Jun 25. doi: 10.1021/acs.jmedchem.5c00928.
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