Chemical Name: N-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)-12-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)-12-oxododecanamide
Biological ActivitySK 575 is a potent PARP1 Degrader (PROTAC®; DC50 ≤ 6.72 nM, >99% PARP1 degradation at 10 nM). It comprises the PARP1/2 inhibitor Olaparib (Cat. No. 7579), joined by a linker to cereblon/cullin 4A ligand Thalidomide (Cat. No. 0652). SK 575 inhibits the growth of various cancer cell lines bearing BRCA1/2 mutations with IC50 values in the nanomolar range. It effectively reduces PARP1 protein levels in mouse SW620 tumor xenograft models. SK 575 dose-dependently potentiates the antitumor activity of Temozolomide (Cat. No. 2706) and Cisplatin (Cat. No. 2251) in vivo.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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