aladdin 阿拉丁 A413926 AMG 337 1173699-31-4 98%

中文名：AMG 337

英文名：AMG 337

纯度：Moligand™，≥98%

货号：A413926

Cas号：1173699-31-4

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

AMG 337 AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the Met (c-Met) receptor with an IC50 of 1 nM.

Targets

MET receptor (Cell-free assay); MET(H1094R) (Cell-free assay); MET(M1250T) (Cell-free assay); MET(V1092I) (Cell-free assay) 1 nM; 1 nM ;4.7 nM; 21.5 nM

In vitro

AMG 337 potently inhibits the enzymatic activity of WT MET and a subset of MET mutants found in papillary renal cell carcinoma. The inability of AMG 337 to inhibit the Y1230 and D1228 mutants is likely the result of a disruption of the inactive confirmation of the activation loop in the MET kinase domain. AMG 337 also inhibits cell based HGF-induced MET phosphorylation in PC3 cells with IC50 of 5nM.AMG 337 inhibits proliferation in MET-dependent cancer cell lines. AMG 337 inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines resulting in profound effects on cell proliferation and survival.

In vivo

AMG 337 exhibits impressive potency with >90% inhibition of Gab-1 phosphorylation at a dose of 0.75 mg/kg (32 nmol/L free-drug concentration). AMG 337 is well tolerated at continuously administered doses that corresponded with complete MET inhibition for 24 hours, suggesting that AMG 337 has the preclinical attributes required to test the role of MET in human cancer.

Cell Research(from reference)

Cell lines：Human cancer cell lines 

Concentrations：serial dilution(a top concentration of 3 mmol/L.) 

Incubation Time：72 h 

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