SBI-0206965

Modify Date: 2024-01-13 13:04:37

SBI-0206965 Structure
SBI-0206965 structure
Common Name SBI-0206965
CAS Number 1884220-36-3 Molecular Weight 489.319
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C21H21BrN4O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of SBI-0206965


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 .IC50 value: 108nM/711 nMTarget: ULK1/ ULK2in 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.

 Names

Name SBI-0206965
Synonym More Synonyms

 SBI-0206965 Biological Activity

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 .IC50 value: 108nM/711 nMTarget: ULK1/ ULK2in 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.
Related Catalog
References

[1]. Egan DF, et al. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates. Mol Cell. 2015 Jul 16;59(2):285-297.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C21H21BrN4O5
Molecular Weight 489.319
Exact Mass 488.069519
LogP 3.26
Index of Refraction 1.619
Storage condition -20℃

 Synonyms

2-({5-Bromo-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl}oxy)-N-methylbenzamide
Benzamide, 2-[[5-bromo-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]oxy]-N-methyl-
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