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ONT-993

Names

[ CAS No. ]:
937263-81-5

[ Name ]:
ONT-993

[Synonym ]:
{4-Methyl-2-[(4-{[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]amino}-6-quinazolinyl)amino]-4,5-dihydro-1,3-oxazol-4-yl}methanol
4-Oxazolemethanol, 4,5-dihydro-4-methyl-2-[[4-[[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]amino]-6-quinazolinyl]amino]-

Biological Activity

[Description]:

ONT-993 is an aliphatic hydroxylated metabolite. ONT-993 inhibits CYP2D6 (IC50=7.9 µM) and causes metabolism-dependent inactivation of CYP3A (KI=1.6 µM)[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

[Target]

CYP2D6:7.9 μM (IC50)


[References]

[1]. Sun H, et al. Elimination of tucatinib, a small molecule kinase inhibitor of HER2, is primarily governed by CYP2C8 enantioselective oxidation of gem-dimethyl. Cancer Chemother Pharmacol. 2022 Jun;89(6):737-750.  

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C26H24N8O3

[ Molecular Weight ]:
496.52

[ Exact Mass ]:
496.197144

[ LogP ]:
2.38

[ Index of Refraction ]:
1.742


Related Compounds

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