CZL-046 is a p300 bromodomain inhibitor. CZL-046 shows potent inhibitory activity of p300 bromodomain (IC50 = 3.3 nM) and antiproliferative activity in the multiple myeloma (MM) cell line (OPM-2 IC50 = 51.5 nM). 2 CZL-046 suppressed the mRNA levels of c-Myc and IRF4 and downregulated the expression of c-Myc and H3K27Ac. Compared to the lead compound 5, CZL-046 exhibits significantly improved in vitro and in vivo metabolic properties. Oral administration of CZL-046 with 30 mg/kg achieved a TGI value of 44% in the OPM-2 xenograft model, accompanied by good tolerability.
MedKoo Cat#: 128034
Name: CZL-046
CAS#: 3032444-02-0
Chemical Formula: C29H26D3F3N4O3
Exact Mass: 541.2380
Molecular Weight: 541.59
Elemental Analysis: C, 64.31; H, 5.95; F, 10.52; N, 10.35; O, 8.86
The following data is based on the product molecular weight 541.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
