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Merestinib dihydrochloride

Product Specifications

UNSPSC Description

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].

Target Antigen

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

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 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.Methods Mol Biol. 2018;1711:351-398.|bioRxiv. 2024 May 8:2024.05.07.592424.|Cancer Discov. 2016 Dec;6(12):1334-1341.|Clin Cancer Res. 2020 Jun 1;26(11):2615-2625.|Patent. WO2017019702A1.

Shipping Conditions

Room Temperature

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-15514A/Merestinib-dihydrochloride-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-15514A/Merestinib-dihydrochloride-SDS-MedChemExpress.pdf

Clinical Information

Phase 2

CAS Number

1206801-37-7

Available Sizes

Curated Selection

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