DDO-8958 is a BET BD1-Selective Inhibitor for Pancreatic Cancer Therapy. DDO-8958 exhibited a KD of 5.6 nM for BRD4 BD1 and a 214-fold selectivity for BRD4 BD1 over BD2. DDO-8958 extensively influenced the oncogene expression and metabolic pathway, including oxidative phosphorylation in MIA PaCa-2. In vivo, DDO-8958 inhibited tumor growth and markedly augmented the therapeutic efficacy of the glycolysis inhibitor 2-DG. These findings illuminate that multi-water bridges enable design of BD1-selective inhibitors and a therapeutic strategy involving combined targeting of BD1-induced epigenetic reprogramming and glycolysis pathways for the management of pancreatic cancer.
MedKoo Cat#: 128555
Name: DDO-8958
CAS#: N/A
Chemical Formula: C22H22FN5O2
Exact Mass: 407.1758
Molecular Weight: 407.45
Elemental Analysis: C, 64.85; H, 5.44; F, 4.66; N, 17.19; O, 7.85
The following data is based on the product molecular weight 407.45 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 |
