| Identification | Back Directory | [Name]
2H-Benzimidazol-2-one, 5-[[5-chloro-2-[(3R,5S)-4,4-difluoro-3,5-dimethyl-1-piperidinyl]-4-pyrimidinyl]amino]-1,3-dihydro-3-(3-hydroxy-3-methylbutyl)-1-methyl- | [CAS]
2647503-57-7 | [Synonyms]
2H-Benzimidazol-2-one, 5-[[5-chloro-2-[(3R,5S)-4,4-difluoro-3,5-dimethyl-1-piperidinyl]-4-pyrimidinyl]amino]-1,3-dihydro-3-(3-hydroxy-3-methylbutyl)-1-methyl- | [Molecular Formula]
C24H31ClF2N6O2 | [MOL File]
2647503-57-7.mol | [Molecular Weight]
508.99 |
| Chemical Properties | Back Directory | [Boiling point ]
640.1±65.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
15.14±0.29(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
CCT369260 (compound 1) is an orally avtive B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity. CCT369260 (compound 1) exhibits an IC50 of 520 nM[1]. | [in vivo]
CCT369260 (compound 1, 15 mg/kg, po, single dose) significantly inhibits BCL6 in OCI-Ly1 DLBCL xenograft model[1]. | Animal Model: | OCI-Ly1 DLBCL xenograft model (female SCID mice)[1]. | | Dosage: | 15 mg/kg. | | Administration: | PO, single dose. | | Result: | Decreased the levels of BCL6 in the tumor observed up to 10 h after administration. |
| Animal Model: | Female Balb/C mice[1]. | | Dosage: | 1 mg/kg iv and 5 mg/kg po (Pharmacokinetic Analysis). | | Administration: | IV and PO | | Result: | Demonstrated moderate clearance (CL 20 mL min?1 kg?1) with mean oral bioavailability of 54%. |
| [References]
[1] Benjamin R Bellenie, et al. Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders. J Med Chem. 2020 Apr 23;63(8):4047-4068. DOI:10.1021/acs.jmedchem.9b02076 |
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