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c-MET inhibitor 7

Chemical Structure : c-MET inhibitor 7

CAS No.:

c-MET inhibitor 7

Catalog No.: PC-49280Not For Human Use, Lab Use Only.

c-MET inhibitor 7 is a potent, highly selective c-MET inhibitor with IC50 of 0.90 and 0.09 μM for wild-type and D1228V c-MET, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

c-MET inhibitor 7 is a potent, highly selective c-MET inhibitor with IC50 of 0.90 and 0.09 μM for wild-type and D1228V c-MET, respectively.
c-MET inhibitor 7 binds to the hinge region via its indazole group and extending into the back pocket, with significant rearrangement of the back pocket and αC helix residues.
c-MET inhibitor 7 is highly selective, inhibit justs 3 kinases out of a panel of 140 to any significant degree (i.e. >70%).
c-MET inhibitor 7 inhibits D1228V c-MET activity in a cellular system using a homogenous time-resolved FRET target-engagement assay with IC50 of 12 uM.

Physicochemical Properties

M.Wt 460.529
Formula C27H26F2N4O
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

Chemical Name/SMILES

(R)-3-(difluoromethyl)-N-methyl-N-(8-methyl-5-(3-methyl-1H-indazol-6-yl)-1,2,3,4-tetrahydronaphthalen-1-yl)picolinamide

References

1. Gavin W Collie, et al. Bioorg Med Chem Lett. 2022 Aug 17;128948.

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