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MS 28

Cat. No. 8076 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： Cyclin D1, CDK4/6 and cyclin D3 Degrader (PROTAC®)
化学名： (2S,4R)-1-((S)-2-(7-(4-(6-((6-Acetyl-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazin-1-yl)-7-oxoheptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
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 MS 28

MS 28 is a cyclinD1 Degrader (PROTAC®) (DC50 = 950 nM; Dmax = 90% in vitro). Also degrades CDK4, CDK6 and cyclin D3 after 4 hours. Degrades cyclin D1 and cyclin D3 by recruiting the CDK4/6 as a 'bridge'. Comprises a CDK4/6 binding moiety joined by a linker to a VHL ligand. Suppresses NCI-H2110 and Calu-1 cancer cell growth at 1 μM.

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

许可信息

Sold under license from Icahn School of Medicine at Mount Sinai.

技术数据 for MS 28

分子量 1002.25
公式 C53H67N11O7S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2229974-73-4
PubChem ID 146014438
InChI Key MWVNDEBEHBRZEC-WWTLGBROSA-N
Smiles O=C1N(C2CCCC2)C3=NC(NC4=CC=C(N5CCN(CC5)C(CCCCCC(N[C@@H](C(C)(C)C)C(N6[C@@H](C[C@H](C6)O)C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)=O)=O)=O)C=N4)=NC=C3C(C)=C1C(C)=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 MS 28

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 100.22 100

制备储备液 for MS 28

以下数据基于产品分子量 1002.25。 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 mL 4.99 mL 9.98 mL
5 mM 0.2 mL 1 mL 2 mL
10 mM 0.1 mL 0.5 mL 1 mL
50 mM 0.02 mL 0.1 mL 0.2 mL

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参考文献 for MS 28

参考文献是支持产品生物活性的出版物。

Xiong et al (2022) Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets. J.Am.Chem.Soc. 144 22622 PMID: 36448571

If you know of a relevant reference for MS 28, please let us know.

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关键词: MS 28, MS 28 supplier, MS28, degrader, degrades, degraders, protac, proteolysis, chimera, cdk, cdk4, cdk6, cyclin, cyclind1, cyclind3, bridge, VHL, von, hippel, lindau, E3, ligase, Cyclin, Dependent, Kinase, (CDK), Degraders, 8076, 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