BiochemProbe — Life Science Research Reagents

LY2801653 free base · Synonyms: LY-2801653 · LY 2801653

Merestinib is a potent, orally bioavailable c-Met inhibitor.

For research use only. Not for human or veterinary use.

Target c-Met/HGFR FLT3 ROS Kinase Discoidin Domain Receptor
Research area Cancer
Purity >98% Stock Inquire
Data Sheet SDS COA

LY2801653 structure

CAS No.: 1206799-15-6

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
250 mg USD 480.00 BP-02132-250mg In stock Get quote
500 mg USD 760.00 BP-02132-500mg In stock Get quote
1 g USD 1,220.00 BP-02132-1g In stock Get quote
2 g USD 1,950.00 BP-02132-2g In stock Get quote
3 g USD 2,800.00 BP-02132-3g In stock Get quote
5 g USD 3,800.00 BP-02132-5g In stock Get quote

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Description

Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) 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) .

Biological activity

In Vitro Merestinib (LY2801653) demonstrates effects on MET pathway-dependent cell scattering and cell proliferation. The mean IC50 value (n=6 determinations) of Merestinib (LY2801653) for inhibition of MET auto-phosphorylation in HGF-stimulated H460 cells is 35.2±6.9 nM and the IC50 for MET auto-phosphorylation in S114 cells is 59.2 nM. Merestinib (LY2801653) also inhibits MST1R (IC50=11 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TYRO3 (IC50=28 nM), ROS1, PDGFRA (IC50=41 nM), FLT3 (IC50=7 nM), TEK (IC50=63 nM), DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM)[1]. Transfection with the MET variants confers growth-factor independence and treatment with Merestinib (LY2801653) inhibits growth of these MET variant clones with an IC50 ranging from 3-fold more potent (V1092I) to approximately 6-fold less potent (L1195V) compare with the growth inhibition of cells with the MET wild-type sequence[1]. Merestinib (LY2801653) (2, 5, and 10 μM) reduces the number of viable TFK-1 and SZ-1 cells in a dose and time dependent manner, and significant inhibits wound healing for TFK-1 and SZ-1 cell lines. Merestinib (LY2801653) inhibits cell invasion in TFK-1 and SZ-1 cells in a concentration dependent manner. 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[1]. 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.

Identifiers

SMILES
CN1N=CC2=C1C=C(C1=CNN=C1)C(OC1=CC=C(NC(=O)C3=CC=C(C)N(C3=O)C3=CC=C(F)C=C3)C=C1F)=C2
InChIKey
QHADVLVFMKEIIP-UHFFFAOYSA-N

Specifications

MW (average)
552.5309
Formula
C30H22F2N6O3
CAS No.
1206799-15-6
Physical state
Solid
Color
White to yellow
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[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.

Same target

Search c-Met/HGFR

Same research area

Search Cancer