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TD-802

Chemical Structure : TD-802

CAS No.: 2760703-21-5

TD-802 (TD802)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 957.57
Formula C52H61ClN10O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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