| Identification | Back Directory | [Name]
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 2,3,9-trimethyl-4-[3′-[(pyrazolo[1,5-a]pyrimidin-3-ylcarbonyl)amino][1,1′-biphenyl]-4-yl]-, (6S)- | [CAS]
2851986-76-8 | [Synonyms]
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 2,3,9-trimethyl-4-[3′-[(pyrazolo[1,5-a]pyrimidin-3-ylcarbonyl)amino][1,1′-biphenyl]-4-yl]-, (6S)- | [Molecular Formula]
C32H27N9O2S | [MOL File]
2851986-76-8.mol | [Molecular Weight]
601.68 |
| Hazard Information | Back Directory | [Uses]
PLX-3618 is a molecular glue, that degrades BRD4 with DC50 of 12.2 nM. PLX-3618 promotes polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting of the E3 ligase substrate receptor, DCAF11. PLX-3618 inhibits the proliferation of various cancer cells, induces apoptosis in AML cells. PLX-3618 exhibits antitumor activity against AML in mouse models[1]. | [References]
[1] Parker GS, et al., Discovery of Monovalent Direct Degraders of BRD4 That Act Via the Recruitment of DCAF11. Mol Cancer Ther. 2024 Jun 22. DOI:10.1158/1535-7163.MCT-24-0219 |
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