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Chemical Structure : Merestinib
CAS No.: 1206799-15-6
Catalog No.: PC-20333Not For Human Use, Lab Use Only.
Merestinib (LY2801653) is a potent, selective, type-II ATP competitive inhibitor of c-Met with Ki of 2 nM, inhibits c-MET wt and mutant Y1230C with IC50 of 42 and 54 nM, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $88 | In stock | |
| 10 mg | $128 | In stock | |
| 25 mg | $218 | In stock | |
| 50 mg | $358 | In stock | |
| 100 mg | Get quote |
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Merestinib (LY2801653) is a potent, selective, type-II ATP competitive inhibitor of c-Met with Ki of 2 nM, inhibits c-MET wt and mutant Y1230C with IC50 of 42 and 54 nM, respectively.
LY2801653 inhibited MET auto-phosphorylation in HGF-stimulated H460 cells and S114 cells with IC50 of 35.2 and 59.2 nM, resepctively.
LY2801653 inhibited growth of a panel of MET mutated variant clones with an IC50 ranging from 3-fold more potent (V1092I) to approximately 6-fold less potent (L1195V) compared with the growth inhibition of cells with the MET wild-type sequence.
LY2801653 demonstrated more potent anti-proliferative activity in cell lines with MET gene amplification (MKN45, Hs746T and H1993) than the cell lines without MET gene amplification (U-87MG, KATO-III).
LY2801653 (12 mg/kg, BID, oral) demonstrated in vivo anti-tumor activity in MET-dependent U-87MG and H441 xenograft models.
| M.Wt | 552.54 | |
| Formula | C30H22F2N6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-[3-fluoro-4-[[1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl]oxy]phenyl]-1-(4-fluorophenyl)-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarboxamide |
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1. Yan SB, et al. Invest New Drugs. 2013 Aug;31(4):833-44.
2. Wu W, et al. Clin Cancer Res. 2013 Oct 15;19(20):5699-710.
3. Kawada I, et al. Cancer Res. 2014 Feb 1;74(3):884-95.
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