Chemical Structure : CBPD-409
货号: PC-22054Not For Human Use, Lab Use Only.
CBPD-409 (CBPD409) is a highly potent, selective, and orally bioavailable CBP/p300 degrader with DC50 0.2-0.4 nM in VCaP, LNCaP, and 22Rv1 AR+ prostate cancer cell lines.
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CBPD-409 (CBPD409) is a highly potent, selective, and orally bioavailable CBP/p300 degrader with DC50 0.2-0.4 nM in VCaP, LNCaP, and 22Rv1 AR+ prostate cancer cell lines.
CBPD-409displays strong antiproliferative effects with IC50 1.2-2.0 nM in the VCaP, LNCaP, and 22Rv1 AR+ prostate cancer cell lines.
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 thanCBP/p300 inhibitors CCS1477 and GNE-049 and the AR antagonist Enzalutamide.
分子量 | 862.98 | |
分子式 | C46H52F2N10O5 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Zhixiang Chen, et al. J Med Chem. 2024 Mar 26.
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