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LY 2801653
- Merestinib
- Soluble in DMSO
- MF: C30H22F2N6O3
- MW: 552.53
Description
Orally bioavailable multi-kinase inhibitor with potent activity against c-MET (IC50 values 35 - 53 nM for cell-based activity), and several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1, DDR2 and against the serine/threonine kinases MKNK1 and MKNK2 (IC50 values 11, 7, 2, 10, 63, 23, 0.1, 7, 7, and 7 nM, respectively). In classic and orthotopic mouse xenograft models of lung cancer, LY2801653 decreased tumor growth, dramatically inhibiting mitotic events and angiogenesis.
More Information
| Parent CAS No. | 1206799-15-6 |
|---|---|
| Chemical Name | N-(3-fluoro-4-(1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yloxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide |
| SMILES | C1(=O)N(C2=CC=C(F)C=C2)C(C)=CC=C1C(NC1=CC=C(OC2C(C3=CNN=C3)=CC3=C(C=2)C=NN3C)C(F)=C1)=O |
| MFCD | MFCD26142925 |
| InChi | InChI=1S/C30H22F2N6O3/c1-17-3-9-23(30(40)38(17)22-7-4-20(31)5-8-22)29(39)36-21-6-10-27(25(32)12-21)41-28-11-18-16-35-37(2)26(18)13-24(28)19-14-33-34-15-19/h3-16H,1-2H3,(H,33,34)(H,36,39) |
| InChiKey | QHADVLVFMKEIIP-UHFFFAOYSA-N |
| CID | 44603533 |
| Short Description | Multi-kinase (c-MET) inhibitor |
References
- SB Yan 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.
- W Wu et al. Inhibition of tumor growth and metastasis in non-small cell lung cancer by LY2801653, an inhibitor of several oncokinases, including MET. Clin Cancer Res. 2013 Oct 15;19(20):5699-710.
- I. Kawada et al. Dramatic antitumor effects of the dual MET/RON small-molecule inhibitor LY2801653 in non-small cell lung cancer. Cancer Res. 2014 Feb 1;74(3):884-95.
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