Chemical Structure : CZL-077
CAS No.:
3032444-06-4
CZL-077
(CZL077)
Catalog No.: PC-25946Not For Human Use, Lab Use Only.
CZL-077 is a potent, selective and orally active p300/CBP bromodomain inhibitor with IC50 of 34 nM and 52 nM respectively, selective over BRD4 BD1 and BD2.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
CZL-077 is a potent, selective and orally active p300/CBP bromodomain inhibitor with IC50 of 34 nM and 52 nM respectively, selective over BRD4 BD1 and BD2.
CZL-077 effectively inhibits cell growth with IC50 values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively.
CZL-077 exhibits high selectivity over the BRDs of BET proteins.
CZL-077 shows potent in vivo efficacy in the OPM-2 xenograft model and demonstrates more potent antitumor activity in the 22RV1 xenograft model, with tumor growth inhibition values of 56.2% and 72.8%, respectively
Physicochemical Properties
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M.Wt
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577.63
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Formula
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C30H26F3N5O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(3S,5S)-1-(3,4-difluorophenyl)-5-(5-(3,5-dimethylisoxazol-4-yl)-1-((R)-2-methyl-4,5,6,7-tetrahydrobenzo[d]thiazol-6-yl)-1H-benzo[d]imidazol-2-yl)-3-fluoropyrrolidin-2-one
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References
1. Chen Z, et al. Eur J Med Chem. 2025 Dec 16;304:118489.
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