SK 575

Key Product Details

Product Description

SK 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.

PARP antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF-600-NA and MAB8095.

PROTAC^® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Product Specifications for SK 575

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for SK 575

The following data is based on the product molecular weight 876.99.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.14 mL	5.70 mL	11.40 mL
5 mM	0.23 mL	1.14 mL	2.28 mL
10 mM	0.11 mL	0.57 mL	1.14 mL
50 mM	0.02 mL	0.11 mL	0.23 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Cao Discovery of SK-575 as a highly potent and efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for treating cancers. J.Med.Chem. 2020 PMID: 32924477

Product Documents for SK 575