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MS 154

Cat. No. 7395 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 and selective cereblon-recruiting Degrader (PROTAC®) of mutant EGFR
化学名： 3-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-N-(8-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)octyl)propanamide
纯度： ≥98% (HPLC)
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引用文献
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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 154

MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib (Iressa, Cat. No. 3000). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50 values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax > 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.

Negative control (Cat. No. 7396) and EGFR antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF231.

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 154

分子量 901.43
公式 C46H54ClFN8O8
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2550393-21-8
PubChem ID 145996534
InChI Key ALKKWBPMCDDKKA-UHFFFAOYSA-N
Smiles COC1=CC2=C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)C=C1OCCCN4CCN(CC4)CCC(NCCCCCCCCOC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=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 154

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 90.14 100

制备储备液 for MS 154

以下数据基于产品分子量 901.43。 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 1.11 mL 5.55 mL 11.09 mL
5 mM 0.22 mL 1.11 mL 2.22 mL
10 mM 0.11 mL 0.55 mL 1.11 mL
50 mM 0.02 mL 0.11 mL 0.22 mL

Molarity Calculator

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参考文献 for MS 154

参考文献是支持产品生物活性的出版物。

Cheng et al (2020) Discovery of potent and selective epidermal growth factor receptor (EGFR) bifunctional small-molecule degraders. J.Med.Chem. 63 1216 PMID: 31895569

If you know of a relevant reference for MS 154, please let us know.

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关键词: MS 154, MS 154 supplier, MS154, potent, selective, mutant, EGFR, active, degraders, degrades, Gefitinib, Iressa, epidermal, growth, factor, receptors, cereblon, CRBN, E3, ligases, targeted, protein, degradation, TPD, PROTACs, Receptor, Degraders, 7395, 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