Identification | Back Directory | [Name]
[1,4]Oxazepino[2,3-c]quinolin-6(7H)-one, 10-[[5-chloro-2-[(3R,5S)-3-hydroxy-5-methyl-1-piperidinyl]-4-pyrimidinyl]amino]-2-cyclopropyl-3,3-difluoro-1,2,3,4-tetrahydro-7-methyl-, (2S)- | [CAS]
2378853-66-6 | [Synonyms]
CCT373566 [1,4]Oxazepino[2,3-c]quinolin-6(7H)-one, 10-[[5-chloro-2-[(3R,5S)-3-hydroxy-5-methyl-1-piperidinyl]-4-pyrimidinyl]amino]-2-cyclopropyl-3,3-difluoro-1,2,3,4-tetrahydro-7-methyl-, (2S)- | [Molecular Formula]
C26H29ClF2N6O3 | [MOL File]
2378853-66-6.mol | [Molecular Weight]
547 |
Chemical Properties | Back Directory | [Boiling point ]
704.8±70.0 °C(Predicted) | [density ]
1.50±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
14.34±0.40(Predicted) | [color ]
Light yellow to yellow |
Hazard Information | Back Directory | [Description]
CCT373566 is a highly potent BCL6 degrader (IC50 =0.7 nM) suitable for sustained depletion of BCL6 in vivo. CCT373566 showed modest in vivo efficacy in a lymphoma xenograft mouse model following oral dosing. The transcriptional repressor BCL6 is an oncogenic driver found to be deregulated in lymphoid malignancies. | [in vitro]
The antiproliferative activity of the degrader CCT373566 and the inhibitor CCT373567 was tested in a panel of cell lines (Table 5). The degradation of BCL6 by CCT373566 translated into potent antiproliferative activity._x000D_
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Reference: J Med Chem. 2022 Jun 23;65(12):8191-8207. https://pubmed.ncbi.nlm.nih.gov/35653645/ | [target]
CCT373566 is a potent and orally active degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. |
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