SK 575

Name: SK 575
Brand: Tocris Bioscience
SKU: 7583

Tocris Bioscience, part of Bio-Techne | Catalog # 7583

COA / SDS

Potent PARP1 Degrader (PROTAC®)

Key Product Details

Description:	Potent PARP1 Degrader (PROTAC^®)
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
Purity:	≥98% (HPLC)
Molecular Weight:	876.99

View Full Technical Details for SK 575

Technical Data
Citations

Biological Activity for SK 575

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.

Technical Data for SK 575

M. Wt	876.99
Formula	C₄₇H₅₃FN₈O₈
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2523016-96-6
PubChem ID	162664494
InChi Key	HPBWDZVXFSTVMR-UHFFFAOYSA-N
Smiles	FC1=CC=C(C=C1C(N2CCN(C(CCCCCCCCCCC(NCCNC3=C4C(N(C(C4=CC=C3)=O)C5CCC(NC5=O)=O)=O)=O)=O)CC2)=O)CC6=NNC(C7=CC=CC=C67)=O

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.

Solubility for SK 575

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	87.7	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for SK 575

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