Chemical Structure : CZL-046
CAS No.:
3032444-02-0
CZL-046
(CZL046)
Catalog No.: PC-23754Not For Human Use, Lab Use Only.
CZL-046 is a potent, selective, and orally active p300 bromodomain inhibitor with IC50 of 3.3 nM, exhibits antiproliferative activity in the multiple myeloma (MM) cell line (OPM-2, IC50=51.5 nM).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
CZL-046 is a potent, selective, and orally active p300 bromodomain inhibitor with IC50 of 3.3 nM, exhibits antiproliferative activity in the multiple myeloma (MM) cell line (OPM-2, IC50=51.5 nM).
CZL-046 shows slightly higher selectivity over the bromodomains of BET proteins than CCS1477, especially BD2 with IC50 values greater than 9 μM.
CZL-046 suppresses the mRNA levels of c-Myc and IRF4 and downregulated the expression of c-Myc and H3K27Ac, exhibits intracellular H3K27Ac inhibitory activity with IC50 of 109 nM in OPM-2 cell line.
CZL-046 induces apoptosis and cell cycle G0/G1 phase arrest in OPM-2 cells
CZL-046 significantly inhibited the growth of the tumor with 30 mg/kg oral administration following 21 days of once-daily dosing in OPM-2 xenograft model.
Physicochemical Properties
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M.Wt
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541.59
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Formula
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C29H26D3F3N4O3
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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-((1r,4S)-4-(methoxy-d3)cyclohexyl)-1H-benzo[d]imidazole-2-yl)-3-fluoropyrrolidin-2-one
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References
1. Chen Z, et al. J Med Chem. 2024 Oct 24;67(20):18606-18628.
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