LY2801653 dihydrochloride

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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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Our Products Cannot Be Used As Medicines Directly For Personal Use.

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