Chemical Structure : MET inhibitor 13
CAS No.:
MET inhibitor 13
Catalog No.: PC-22805Not For Human Use, Lab Use Only.
MET inhibitor 13 is a potent, selective and mutant-active MET kinase inhibitor with IC50 of 6/6 nM for D1228N/exon Δ14 enzyme, and 90/15/5 nM for F1200I/L1995 V/Y1230H mutants respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
MET inhibitor 13 is a potent, selective and mutant-active MET kinase inhibitor with IC50 of 6/6 nM for D1228N/exon Δ14 enzyme, and 90/15/5 nM for F1200I/L1995 V/Y1230H mutants respectively.
MET inhibitor 13 displayed inhibition of only 5 kinases below 50% POC at 1 mM ATP against a panel of 396 kinases.
MET inhibitor 13 (30 mg/kg BID, oral) demonstrated antitumor activity in the subcutaneous Hs746T MET exon 14/MET amplified xenograft model.
Physicochemical Properties
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M.Wt
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612.58
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Formula
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C30H23F3N10O2
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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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N-(2,5-Difluoro-4-((trans-3-(1-methyl-1H-pyrazol-3-yl)cyclobutyl)(pyrazolo[1,5-a]pyrazin-4-yl)amino)phenyl)-2-(5-fluoropyridin-2-yl)-3-oxo-2,3-dihydropyridazine-4-carboxamide
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References
1. Bumpers QA, et al. J Med Chem. 2024 Aug 1. doi: 10.1021/acs.jmedchem.4c01232.
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