CBPD-409 is a highly potent, selective, and orally bioavailable CBP/p300 degrader. CBPD-409 induces robust CBP/p300 degradation with DC50 0.2−0.4 nM and displays strong antiproliferative effects with IC50 1.2−2.0 nM in the VCaP, LNCaP, and 22Rv1 AR+ prostate cancer cell lines. It has a favorable pharmacokinetic profile and achieves 50% of oral bioavailability in mice. A single oral administration of CBPD-409 at 1 mg/kg achieves >95% depletion of CBP/p300 proteins in the VCaP tumor tissue. CBPD-409 exhibits strong tumor growth inhibition and is much more potent and efficacious than two CBP/p300 inhibitors CCS1477 and GNE-049 and the AR antagonist Enzalutamide.
MedKoo Cat#: 126625
Name: CBPD-409
CAS#: N/A
Chemical Formula: C46H52F2N10O5
Exact Mass: 862.4090
Molecular Weight: 862.98
Elemental Analysis: C, 64.02; H, 6.07; F, 4.40; N, 16.23; O, 9.27
The following data is based on the product molecular weight 862.98 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 |
