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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Met (HGFR)-Merestinib
Merestinib

Chemical Structure : Merestinib

CAS No.: 1206799-15-6

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Merestinib (LY2801653, LY-2801653)

货号: 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.

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10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2580 In stock
100 mg ￥4280 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 552.54
分子式 C30H22F2N6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
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

参考文献

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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