Home Protein Tyrosine Kinase TAM receptors (Tyro-3,Axl,and Mertk) inhibitor Merestinib dihydrochloride

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Merestinib dihydrochloride TAM receptors (Tyro-3,Axl,and Mertk) inhibitor

Cat.No.E7462

Merestinib dihydrochloride (LY2801653 dihydrochloride) is an orally bioavailable, potent c-Met inhibitor exhibiting a Ki value of 2 nM. This compound demonstrates antitumor activity and inhibits multiple kinases, including 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).
Merestinib dihydrochloride TAM receptors (Tyro-3,Axl,and Mertk) inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 625.45

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Chemical Information, Storage & Stability

Molecular Weight 625.45 Formula

C30H24Cl2F2N6O3

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CAS No. 1206801-37-7 Download SDF Storage of Stock Solutions

Synonyms LY2801653 dihydrochloride 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

Mechanism of Action

In vivo
Merestinib (LY2801653) demonstrates 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. Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a pharmacodynamic residence time (Koff) of 0.00132 min-1 and t1/2 of 525 min. Merestinib (LY2801653) treatment inhibits MET phosphorylation with a composite TED50 (50 % target inhibition dose) of 1.2 mg/kg and a composite TED90 (90 % target inhibition dose) of 7.4 mg/kg. Merestinib (LY2801653) (20 mg/kg) reduces TFK-1 tumor growth significantly relative to vehicle control. Merestinib (LY2801653) inhibits the growth of intra- and extrahepatic CCC xenograft tumors.
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