AMG458

AMG458

参考价：¥2057
供货周期： 一周
品牌：
规格： 2mg
货号： K1336
CAS号： 913376-83-7
上海高创化学科技有限公司
银牌会员 丨 7年 丨 生产商
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Information
SKU:K1336   M. Wt:539.58  
Formula:C30H29N5O5   Solubility:No  
Purity:>99%   Storage:2 years at -20 degrees centigrade  
CAS No.:913376-83-7   Synonyms:N/A  
Chemical NameN/A
Biological Activity
Description AMG458
Targets human c-Met mouse c-Met      
IC50 1.2 nM(Ki) 2.0 nM(Ki)      
In vitro AMG 458 can potently inhibit human c-Met and mouse c-Met with Ki of 1.2 nM or 2.0 nM. AMG-458 enhances radiosensitivity in H441 but not in A549. A549 expresses low levels of c-Met, which were phosphorylated only in the presence of exogenous hepatocyte growth factor. The combination of radiation therapy and AMG-458 treatment synergistically increase apoptosis in the H441 cell line but not in A549. Radiation therapy, AMG-458, and combination treatment were found to reduce p-Akt and p-Erk levels in H441 but not in A549. H441 became less sensitive to AMG-458 after small interfering RNA knockdown of c-Met; there was no change in A549. After overexpression of c-Met, A549 became more sensitive, while H441 became less sensitive to AMG-458. AMG-458 is more effective in cells that expressed higher levels of c-Met/p-Met.[1]
In vivo N/A
Clinical Trials N/A
Features N/A

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