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2642231-19-2

2642231-19-2 Structure

2642231-19-2 Structure
IdentificationBack Directory
[Name]

PTD10
[CAS]

2642231-19-2
[Synonyms]

PTD10
4-((2-((S)-4-(6-((2'-(7,7-Dimethyl-1-oxo-1,3,4,6,7,8-hexahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-2-yl)-3'-(hydroxymethyl)-1-methyl-6-oxo-1,6-dihydro-[3,4'-bipyridin]-5-yl)amino)pyridin-3-yl)-3-methylpiperazin-1-yl)-2-oxoethyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[(3S)-4-[6-[[2′-(1,3,4,6,7,8-hexahydro-7,7-dimethyl-1-oxo-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-2-yl)-1,6-dihydro-3′-(hydroxymethyl)-1-methyl-6-oxo[3,4′-bipyridin]-5-yl]amino]-3-pyridinyl]-3-methyl-1-piperazinyl]-2-oxoethyl]amino]-
Hazard InformationBack Directory
[Uses]

PTD10 is a highly potent PROTAC BTK degrader (DC50: 0.5 nM, KD: 2.28 nM). PTD10 degrades BTK in Ramos and JeKo-1 cells with DC50s of 0.5 and 0.6 nM respectively. PTD10 inhibits cell growth, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 can be used for research of B-cell dysregulation[1].
[References]

[1] Li YQ, et al. Discovery of Novel Bruton's Tyrosine Kinase PROTACs with Enhanced Selectivity and Cellular Efficacy. J Med Chem. 2023 Jun 8;66(11):7454-7474. DOI:10.1021/acs.jmedchem.3c00176
[2] Li YQ, et, al. Discovery of Novel Bruton's Tyrosine Kinase PROTACs with Enhanced Selectivity and Cellular Efficacy. J Med Chem. 2023 Jun 8;66(11):7454-7474. DOI:10.1021/acs.jmedchem.3c00176
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