INCB054329, also known as INCB-54329, is a potent and selective BET protein inhibitor that targets BD1 and BD2 of BRD2, BRD3 and BRD4. In a panel of colon cancer cell lines, more than 50% are sensitive to INCB054329 treatment with IC50 values below 500 nM in cell proliferation assays. INCB054329 down-regulated c-Myc expression, and induced cell cycle arrest and apoptosis in sensitive colon cancer cell lines. Moreover, INCB54329 was efficacious in the RKO colon cancer xenograft model. INCB054329 as a single agent or in combination with other targeted therapies is potential useful for the treatment of colon cancer.
MedKoo Cat#: 206476
Name: INCB054329
CAS#: 1628607-64-6
Chemical Formula: C19H16N4O3
Exact Mass: 348.1222
Molecular Weight: 348.36
Elemental Analysis: C, 65.51; H, 4.63; N, 16.08; O, 13.78
The following data is based on the product molecular weight 348.36 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 |