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Cell Cycle/Checkpoint ROCK Merestinib dihydrochloride

Merestinib dihydrochloride

Catalog No. T15808   CAS 1206801-37-7
Synonyms: LY2801653 dihydrochloride
Purity 98.00% Datasheet

Merestinib dihydrochloride is an effective and orally bioavailable c-Met inhibitor (Ki=2 nM). It has anti-tumor activities and 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).

Merestinib dihydrochloride, CAS 1206801-37-7
Pack Size Availability Price/USD Quantity
2 mg inquiry 107.00
5 mg inquiry 160.00
10 mg inquiry 258.00
50 mg inquiry 668.00
100 mg inquiry 1079.00
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1 mL * 10 mM (in DMSO) inquiry 219.00
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Merestinib dihydrochloride is an effective and orally bioavailable c-Met inhibitor (Ki=2 nM). It has anti-tumor activities and 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).
Targets&IC50 c-Met :ic50 (ki)2 nM,   MST1R :ic50 11 nM,   FLT3 :ic50 7 nM,   AXL :ic50 2 nM,   MERTK :ic50 10 nM,   TEK :ic50 63 nM,   DDR1/2 :ic50 0.1/7 nM,   MKNK1/2 :ic50 7 nM,  
In vivo Merestinib 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 (20 mg/kg) decreases TFK-1 tumor growth significantly relative to vehicle control. Merestinib 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[1]. Merestinib inhibits the growth of intra- and extrahepatic CCC xenograft tumors[2]. Merestinib 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.
Synonyms LY2801653 dihydrochloride
Purity 98.00%
Appearance solid
Molecular Weight 625.45
Formula C30H24Cl2F2N6O3
CAS No. 1206801-37-7

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 100 mg/mL (159.88 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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.

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