Chemical Structure : CZL-046
货号: 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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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.
分子量 | 541.59 | |
分子式 | C29H26D3F3N4O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Chen Z, et al. J Med Chem. 2024 Oct 24;67(20):18606-18628.
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