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Chemical Structure : CBPD-268
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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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.
| M.Wt | 819.91 | |
| Formula | C44H47F2N9O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Zhixiang Chen, et al. J Med Chem. 2024 Apr 11;67(7):5275-5304.
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