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AMG-47A Catalog No.GC17669

destabilizer of the KRAS oncoprotein

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 882663-88-9 SDF
Chemical Name (Z)-4-methyl-3-((E)-2-((2-morpholinoethyl)imino)-2,3-dihydroquinazolin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzimidic acid
Canonical SMILES CC1=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
Formula C29H28F3N5O2 M.Wt 535.56
Solubility DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 25 mg/ml,Ethanol:PBS (pH 7.2)(1:2): 0.33 mg/ml Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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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]

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