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LY2801653 dihydrochloride
Cat No.
CEI-1408
Product Overview
LY2801653 is a potent, orally bioavailable, small-molecule inhibitor LY2801653 targeting MET kinase. 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).
CAS No.
1206801-37-7
Molecular Weight
625.45
Purity
0.98
Storage
Store at -20°C
Synonyms
LY-2801653 dihydrochloride; LY 2801653 dihydrochloride
Targets
MET
IC50
2 nM (Ki)
Molecular Formula
C30H24Cl2F2N6O3
Chemical Name
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
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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