AMG-47A |
| Catalog No.GC17669 |
L'AMG-47a est un puissant inhibiteur de la protéine tyrosine kinase (Lck) spécifique des lymphocytes et actif par voie orale, avec une CI50 de 0,2 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 882663-88-9
Sample solution is provided at 25 µL, 10mM.
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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]
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
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