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AMG-47A
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AMG-47A图片
CAS NO:882663-88-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
AMG-47a 是一种有效且具有口服活性的淋巴细胞特异性蛋白酪氨酸激酶 (Lck) 抑制剂,IC50 为 0.2 nM。
Cas No.882663-88-9
别名4-甲基-3-[2-[[2-(4-吗啉基)乙基]氨基]-6-喹唑啉基]-N-[3-(三氟甲基)苯基]苯甲酰胺
化学名(Z)-4-methyl-3-((E)-2-((2-morpholinoethyl)imino)-2,3-dihydroquinazolin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzimidic acid
Canonical SMILESCC1=C(C(C=CC2=N/3)=CC2=CNC3=N/CCN4CCOCC4)C=C(/C(O)=N/C5=CC=CC(C(F)(F)F)=C5)C=C1
分子式C29H28F3N5O2
分子量535.56
溶解度DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 25 mg/ml,Ethanol:PBS (pH 7.2)(1:2): 0.33 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AMG-47A is a destabilizer of the KRAS oncoprotein.

Ras is a small GTPase that involves in numerous cellular signaling pathways governing growth, survival, and motility. In humans, there are three Ras genes: KRAS, HRAS, and NRAS. Oncogenic

mutations in all three Ras family members have been identified in human cancers. In particular, KRAS is one of the most frequently mutated oncogenes across cancer types.[1]

In the HeLa EGFP-KRASG12V cells, 48-hour treatment of AMG-47a has a 30–40% decrease in EGFP signal, treating cells for 3 and 5 days shows the similar results. AMG-47a selectively affects EGFP-KRASG12V protein levels. AMG-47a also has a mild effect on EGFP-KRASG12V protein levels after three days. The loss of EGFP-KRASG12V signal plateaus at 50% for AMG-47a. [1]

References:
1. Carver J, Dexheimer TS, Hsu D et al. A high-throughput assay for small molecule destabilizers of the KRASoncoprotein. PLoS One. 2014 Aug 5;9(8):e103836
.