destabilizer of the KRAS oncoprotein
CAS：882663-88-9
分子式：C29H28F3N5O2
分子量：535.56
纯度：98%
存储：Store at -20°C

Background:

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]

参考文献:
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
.