Merestinib dihydrochloride

Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM) [1][2].

Product Specifications

CAS Number

[1206801-37-7]

Product Name Alternative

LY2801653 (dihydrochloride)

UNSPSC

12352005

Target

C-Met/HGFR; Discoidin Domain Receptor; FLT3; ROS Kinase

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/LY2801653-dihydrochloride.html

Concentration

10mM

Purity

99.36

Solubility

DMSO : ≥ 100 mg/mL

Smiles

[H]Cl.[H]Cl.O=C(C1=CC=C(C)N(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=CC5=C(N(C)N=C5)C=C4C6=CNN=C6)C(F)=C3

Molecular Formula

C30H24Cl2F2N6O3

Molecular Weight

625.45

References & Citations

[1]Yan SB, et al. 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. 2013 Aug;31 (4) :833-44.|[2]Barat S, et al. Targeting c-MET by LY2801653 for treatment of cholangiocarcinoma. Mol Carcinog. 2016 Jan 12.