SK 575

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Cat.No. 7583 - SK 575 | C47H53FN8O8 | CAS No. 2523016-96-6
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)
Datasheet
Citations
Reviews
Literature (4)

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.

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 Data for SK 575

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.14 mL 5.7 mL 11.4 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 et al (2020) Discovery of SK-575 as a highly potent and efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for treating cancers. J.Med.Chem. 63 11012 PMID: 32924477


If you know of a relevant reference for SK 575, please let us know.

Keywords: SK 575, SK 575 supplier, SK575, PARP1, Degraders, degrades, PROTAC, Olaparib, BRCA1/2, mutations, targeted, protein, degradation, TPD, Active, Poly(ADP-ribose), Polymerase, 7583, Tocris Bioscience

Citations for SK 575

Citations are publications that use Tocris products.

Currently there are no citations for SK 575. Do you know of a great paper that uses SK 575 from Tocris? Please let us know.

Reviews for SK 575

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Custom Degrader Services
  • Ubiquitin-Proteasome System Proteins and Assays
  • Assays for Protein Degradation
Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia