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MS 143

Cat. No. 8081 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： AKT kinase Degrader (PROTAC®)
化学名： 4-Amino-N-((S)-1-(4-chlorophenyl)-3-(4-(12-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-12-oxododecanoyl)piperazin-1-yl)propyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
纯度： ≥97% (HPLC)
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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 143

MS 143 is a potent and selective AKT kinase Degrader (PROTAC®) (DC50 = 46 nM). MS 143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS 143 suppresses cell growth in prostate cancer PC3 cells. In vivo, MS 143 suppresses tumor growth in a PC3 cell line xenograft mice model.

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 143

分子量 1121.89
公式 C59H81ClN12O6S
储存 Store at -20°C
纯度 ≥97% (HPLC)
CAS Number 2376137-41-4
InChI Key DESJGFOSPPNXOH-XUXNHVGISA-N
Smiles O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(CCCCCCCCCCC(N(CC4)CCN4CC[C@@H](C5=CC=C(C=C5)Cl)NC(C6(CCN(CC6)C7=C8C(NC=C8)=NC=N7)N)=O)=O)=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 143

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 112.19 100

制备储备液 for MS 143

以下数据基于产品分子量 1121.89。 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 0.89 mL 4.46 mL 8.91 mL
5 mM 0.18 mL 0.89 mL 1.78 mL
10 mM 0.09 mL 0.45 mL 0.89 mL
50 mM 0.02 mL 0.09 mL 0.18 mL

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参考文献 for MS 143

参考文献是支持产品生物活性的出版物。

Yu et al (2022) Discovery of potent, selective, and in vivo efficacious AKT kinase protein degraders via structure-activity relationship studies. J.Med.Chem. 65 3644 PMID: 35119851

If you know of a relevant reference for MS 143, please let us know.

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关键词: MS 143, MS 143 supplier, potent, selective, AKT, active, degraders, degrades, PROTAC, PROTACS, targeted, protein, degradation, tpd, in, vivo, PKB, kinase, B, Kinase, Degraders, Akt, (Protein, B), 8081, Tocris Bioscience

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该领域的文献

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

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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