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SBI-0206965

SBI-0206965 ??? ???
?? ??:
1884220-36-3
???:
SBI-0206965
???(??):
CS-1581;SBI-0206965;SBI-0206965（02）;SBI 0206965;SBI0206965;SBI0206965; SBI-0206965; SBI 0206965.;2-((5-Bromo-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)oxy)-N-methylbenzamide;SBI-0206965,SBI 0206965,inhibit,Inhibitor,Unc-51 like kinase,Apoptosis,Autophagy,ULK;Benzamide, 2-[[5-bromo-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]oxy]-N-methyl-
CBNumber:
CB83039306
???:
C21H21BrN4O5
??? ??:
489.32
MOL ??:
1884220-36-3.mol

SBI-0206965 ??

???
170 - 172°C
??
1.434±0.06 g/cm3(Predicted)
?? ??
-20°C
???
DMSO? ???(?? 30mg/ml)
?? ?? (pKa)
14.80±0.46(Predicted)
??? ??
??
??
???? ????
???
??? ?? ?????? 1? ?? ??????. DMSO ??? -20°C?? ?? 3?? ?? ??? ? ????.
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
????(GHS): GHS hazard pictograms
?? ?: Warning
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H315 ??? ??? ??? ????? ?? ????? ?? 2 ?? GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 ?? ?? ??? ??? ?? ? ?? ?? ??? ?? ?? 2A ?? GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 ?? ???? ??? ? ?? ?? ???? ?? - 1? ??;???? ?? ?? 3 ?? GHS hazard pictograms
??????:
P261 ??·?·??·???·??·...·????? ??? ????.
P264 ?? ??? ?? ??? ????.
P264 ?? ??? ?? ??? ????.
P271 ?? ?? ??? ? ?? ???? ?????.
P280 ????/???/???/?????? ?????.
P302+P352 ??? ??? ??? ?? ????.
P305+P351+P338 ?? ??? ? ?? ?? ???? ????. ???? ?????? ?????. ?? ????.
NFPA 704
0
2 0

SBI-0206965 C??? ??, ??, ??

??

ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM). It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells. SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 . It also blocks ULK1-dependent cell survival following nutrient deprivation.

??

SBI-0206965 is an inhibitor of ULK1. It also blocks ULK1-dependent cell survival following nutrient deprivation. ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation.

Biochem/physiol Actions

Since most of the tumor cells survive on autophagy mechanism, inhibition of autophagy inducers Unc-51 (serine/threonine-protein kinase)-like autophagy activating kinase (ULK1 and ULK2) might be useful in cancer therapy.

SBI-0206965 ?? ?? ? ???

???

?? ??

SBI-0206965 ?? ??

???( 86)?? ??
??? ?? ??? ?? ?? ? ??
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SBI-0206965 ?? ??:

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