Chemical Structure : CBPD-409
CAS No.:
CBPD-409
(CBPD409)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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862.98
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Formula
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C46H52F2N10O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-(4-(((1r,4r)-4-(5-Acetyl-3-(7-(difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)cyclohexyl)methyl)piperazin-1-yl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
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References
1. Zhixiang Chen, et al. J Med Chem. 2024 Mar 26.
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