Brief Description

LY2801653 2Hcl is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).
IC50 Value: 2 nM (Ki value)
Target: c-Met
in 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. 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.
Clinical trial: LY2801653 is currently in phase 1 clinical testing in patients with advanced cancer (trial I3O-MC-JSBA, NCT01285037).

Solubility

DMSO

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

White solid