SBI-0206965

Names

[ Name ]:
SBI-0206965

[Synonym ]:
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-

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]:

Signaling Pathways >> Autophagy >> ULK

Research Areas >> Cancer

[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.

[Related Small Molecules]

MRT67307 | MRT-68921 hydrochloride

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℃

Related Compounds

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