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TD-522

Chemical Structure : TD-522

CAS No.: 2417647-40-4

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TD-522 (TD522)

Catalog No.: PC-23948Not For Human Use, Lab Use Only.

TD-522 is a potent, selective GSPT1 degrader, ffectively induces GSPT1 degradation with DC50 of 0.269 nM and Dmax of >95 % at 10 nM in KG-1 cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

TD-522 is a potent, selective GSPT1 degrader, ffectively induces GSPT1 degradation with DC50 of 0.269 nM and Dmax of >95 % at 10 nM in KG-1 cells.
TD-522 exhibits strong anti-proliferative effects in both KG-1 (EC50 = 0.5 nM) and TMD-8 (EC50 = 5.2 nM) cell lines.
Degradation of GSPT1 by TD-522 can increase the accumulation of ATF4 and activate the apoptosis pathway in U-937 cells.
TD-522 (50 mg/kg) effectively suppress TMD-driven tumor growth in xenograft model.

Physicochemical Properties

M.Wt 510.98
Formula C25H27ClN6O4
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

1-(4-(tert-butyl)-3-chlorophenyl)-3-(1-(3-(2,6-dioxopiperidin-3-yl)-4-oxo-3,4-dihydrobenzo[d][1,2,3]triazin-6-yl)ethyl)urea

References

1. Takwale AD, et al. Bioorg Chem. 2022 Oct;127:105923.

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