Chemical Structure : CBPD-268
CAS No.:
2832961-58-5
CBPD-268
(CBPD268)
Catalog No.: PC-22940Not For Human Use, Lab Use Only.
CBPD-268 is a potent, effective, and orally efficacious PROTAC degrader of CBP/p300 proteins DC50 of 0.5 nM against CBP and DC50 of 0.8 nM against p300 and Dmax of 100% against both proteins in the HiBit assays.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
CBPD-268 is a potent, effective, and orally efficacious PROTAC degrader of CBP/p300 proteins DC50 of 0.5 nM against CBP and DC50 of 0.8 nM against p300 and Dmax of 100% against both proteins in the HiBit assays.
CBPD-268 displayed a strong binding affinity against both CBP and p300, with IC50 values of 11 and 9.5 nM, respectively.
CBPD-268 induces the degradation of CBP/p300 proteins in the 22Rv1 cell line with DC50 of <0.03 nM.
CBPD-268 potently and effectively suppressed cell growth with IC50 values of 3.7 nM, 10.3 nM, and 4.6 nM achieved in the 22Rv1, LNCaP, and VCaP cell lines, respectively.
CBPD-268 0.3-3 mg/kg resulted in profound and persistent CBP/p300 depletion in tumor tissues and achieved strong antitumor activity in the VCaP and 22Rv1 xenograft tumor models in mice.
Physicochemical Properties
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M.Wt
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819.91
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Formula
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C44H47F2N9O5
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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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6-((trans-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)-2-(2,6-dioxopiperidin-3-yl)-6,7-dihydropyrrolo[3,4-f]isoindole-1,3(2H,5H)-dione
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References
1. Zhixiang Chen, et al. J Med Chem. 2024 Apr 11;67(7):5275-5304.
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