TD-802 | AR PROTAC | Probechem Biochemicals

Chemical Structure : TD-802

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TD-802 (TD802)

货号: PC-21127Not For Human Use, Lab Use Only.

TD-802 is potent, cereblon-mediated androgen receptor PROTAC degrader, effectively inducs AR protein degradation with DC50 of 12.5 nM and Emax 93% in LNCaP prostate cancer cells.

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生物&药学活性

TD-802 is potent, cereblon-mediated androgen receptor PROTAC degrader, effectively inducs AR protein degradation with DC50 of 12.5 nM and Emax 93% in LNCaP prostate cancer cells.
TD-802 potently inhibits LNCaP and VCaP cell proliferation with IC50 of 98 and 44 nM, respectively.
TD-802 (30 mg/kg, 20% PEG400 + 3% Tween 80 in PBS, i.p., once a day for 10 days) effectively inhibited the growth of AR-positive VCaP prostate in vivo, with no additional loss in body weight or off-target effects.

物理化学性质&存储条件

分子量	957.57
分子式	C52H61ClN10O6
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	N-((1R,3R)-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl)-4-(4-(7-(1-(3-(2,6-dioxopiperidin-3-yl)-4-oxo-3,4-dihydrobenzo[d][1,2,3]triazin-6-yl)piperidine-4-carbonyl)-7-azaspiro[3.5]nonan-2-yl)piperazin-1-yl)benzamide

参考文献

1. Akshay D Takwale, et al. Eur J Med Chem. 2020 Dec 15;208:112769.

TD-802 (TD802)

生物&药学活性

物理化学性质&存储条件

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TD-802 (TD802)

生物&药学活性

物理化学性质&存储条件

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