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首页-抗体药物偶连体和PROTACs-PROTAC-CBPD-409
CBPD-409

Chemical Structure : CBPD-409

CAS No.:

CBPD-409 (CBPD409)

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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 862.98
分子式 C46H52F2N10O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Zhixiang Chen, et al. J Med Chem. 2024 Mar 26.

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