Cas No.: | 1884220-36-3 |
Chemical Name: | 2-((5-bromo-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)oxy)-N-methylbenzamide |
Synonyms: | SBI 0206965,SBI0206965 |
SMILES: | C(NC)(=O)C1=CC=CC=C1OC1C(Br)=CN=C(NC2=CC(OC)=C(OC)C(OC)=C2)N=1 |
Formula: | C21H21BrN4O5 |
M.Wt: | 489.33 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2 |
In Vitro: | SBI-0206965 has very high selectivity, only inhibits 10 out of 456 kinases >95% when tested at 10 μM. SBI-0206965 suppressed ULK1-mediated phosphorylation events in cells, regulating autophagy and cell survival It can suppress autophagy induced by mTOR inhibition, prevent ULK1-dependent cell survival following nutrient deprivation. It greatly synergized with mechanistic target of rapamycin (mTOR) inhibitors to kill tumor cells, providing a strong rationale for their combined use in the clinic. |