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SK 575

Cat. No. 7583 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent PARP1 Degrader (PROTAC®)
化学名： 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
纯度： ≥98% (HPLC)
说明书
引用文献
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文献 (2)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 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.

技术数据 for SK 575

分子量 876.99
公式 C47H53FN8O8
储存 Store at -20°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for SK 575

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 87.7 100

制备储备液 for SK 575

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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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参考文献 for SK 575

参考文献是支持产品生物活性的出版物。

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.

按标靶查看相关产品

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

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该领域的文献

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

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

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
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