LY2801653 dihydrochloride

• CAT Number: I000768
• CAS Number: 1206801-37-7
• Molecular Formula: C30H24Cl2F2N6O3
• Molecular Weight: 625.45
• Purity: ≥95%
• Synonyms: N-[3-fluoro-4-[1-methyl-6-(1H-pyrazol-4-yl)indazol-5-yl]oxyphenyl]-1-(4-fluorophenyl)-6-methyl-2-oxopyridine-3-carboxamide;dihydrochloride
• Target: c-MET
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 2 nM (Ki value) [1]

LY2801653 2Hcl is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).IC50 Value: 2 nM (Ki value) [1]Target: c-Metin vitro: LY2801653 is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (K(i)) of 2 nM, a pharmacodynamic residence time (K(off)) of 0.00132 min(-1) and t(1/2) of 525 min [1]. LY2801653 was found to have potent activity against several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1/2 and against the serine/threonine kinases MKNK1/2.in vivo: LY2801653 demonstrated in vitro effects on MET pathway-dependent cell scattering and cell proliferation; in vivo anti-tumor effects in MET amplified (MKN45), MET autocrine (U-87MG, and KP4) and MET over-expressed (H441) xenograft models; and in vivo vessel normalization effects [1].Clinical trial: LY2801653 is currently in phase 1 clinical testing in patients with advanced cancer (trial I3O-MC-JSBA, NCT01285037).

Reference

[1]. Yan SB, Peek VL, Ajamie R, LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models. Invest New Drugs. 2012 Dec 29. [Epub ahead of print]