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AMG-337 {[allProObj[0].p_purity_real_show]}

货号:A103152

AMG-337 is a potent, highly selective and ATP-competitive MET kinase inhibitor with an IC50 of < 5nM in enzymatic assays.

AMG-337 化学结构 CAS号:1173699-31-4
AMG-337 化学结构
CAS号:1173699-31-4
AMG-337 3D分子结构
CAS号:1173699-31-4
AMG-337 化学结构 CAS号:1173699-31-4
AMG-337 3D分子结构 CAS号:1173699-31-4
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AMG-337 纯度/质量文件 产品仅供科研

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AMG-337 生物活性

描述 The MET receptor tyrosine kinase (RTK) plays a central role in regulating cell growth, survival, and invasion. Binding of hepatocyte growth factor (HGF) promotes MET dimerization, stimulating MET kinase activity. AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the MET receptor. It potently inhibits the enzymatic activity of WT MET (IC50 = 1 nM) and a subset of MET mutants found in papillary renal cell carcinoma. AMG 337 also inhibits cell based HGF-induced MET phosphorylation in PC3 cells (IC50 = 5 nM). Competitive binding assays illustrated the selectivity of AMG 337, binding only MET when profiled against a diverse panel of 402 human kinases. AMG 337 inhibits proliferation in MET-dependent cancer cell lines following 72 hours of treatment with AMG 337. MET phosphorylation was completely inhibited in the gastric cancer cells lines MKN-45, SNU-620, and SNU-5 cells, following a 2-hour treatment with 100 nM AMG 337. In MKN-45 cells, 300 nM AMG 337 treatment for 24 hours resulted in a dose-dependent increase in cells in the G1 phase; with concurrent reduction of cells in S-phase. AMG 337 at a 0.5 mg/kg dose robustly inhibited Gab-1 (a kind of adaptor protein) phosphorylation, and escalation to 0.75 mg/kg or more resulted in >90% inhibition of MET signaling in the TPR-MET mouse tumor model [3].
作用机制 AMG 337 binds to a well-defined, inactive conformation of the MET activation loop (A-loop) in a binding mode .

AMG-337 参考文献

[1]Hughes PE, Rex K, et al. In Vitro and In Vivo Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models. Mol Cancer Ther. 2016 Jul;15(7):1568-79.

[2]Cecchi F, Rabe DC, et al. Targeting the HGF/Met signaling pathway in cancer therapy. Expert Opin Ther Targets. 2012 Jun;16(6):553-72.

[3]Hughes PE, Rex K, Caenepeel S, Yang Y, Zhang Y, Broome MA, Kha HT, Burgess TL, Amore B, Kaplan-Lefko PJ, Moriguchi J, Werner J, Damore MA, Baker D, Choquette DM, Harmange JC, Radinsky R, Kendall R, Dussault I, Coxon A. In Vitro and In Vivo Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models. Mol Cancer Ther. 2016 Jul;15(7):1568-79. doi: 10.1158/1535-7163.MCT-15-0871. Epub 2016 Apr 19. PMID: 27196782.

AMG-337 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.79mL

2.16mL

1.08mL

21.58mL

4.32mL

2.16mL

AMG-337 技术信息

CAS号1173699-31-4
分子式C23H22FN7O3
分子量 463.464
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(226.55 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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