LY2801653 dihydrochloride

Short Summary : MET inhibitor

Category : Tyrosine Kinase|c-MET

Purity : 0.98

CAS Number : 1206801-37-7

Formula : C30H24Cl2F2N6O3

Molecular Weight : 625.45

SMILE : CC1=CC=C(C(=O)N1C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C(C=C5C(=C4)C=NN5C)C6=CNN=C6)F.Cl.Cl

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : Description:
IC50 Value: 2 nM(Ki value) [1]
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 [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).

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