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MS 6105

Cat. No. 8073 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 lactate dehydrogenase Degrader (PROTAC®)
化学名： 2-(5-(Cyclopropylmethyl)-3-(3-(6-(13-(((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)-13-oxotridecanamido)hex-1-yn-1-yl)phenyl)-4-(4-sulfamoylbenzyl)-1H-pyrazol-1-yl)thiazole-4-carboxylic acid
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 6105

MS 6105 is a potent and selective lactate dehydrogenase (LDH) Degrader (PROTAC®; for LDHA and LDHB respectively, DC50 values are 38 nM and 74 nM; Dmax is 93% and 86%). Comprises an LDH inhibitor warhead connected by a linker to a VHL ligand. Suppresses growth of several pancreatic cancer cell lines (IC50 range is 12.2 μM - 16.1 μM). Bioavailable in vivo.

技术数据 for MS 6105

分子量 1228.6
公式 C65H81N9O9S3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2891709-58-1
PubChem ID 166642429
InChI Key APEYSKGQWJKJAZ-LCLGPXMOSA-N
Smiles O=C([C@@H](NC(CCCCCCCCCCCC(NCCCCC#CC1=CC=CC(C2=NN(C(CC3CC3)=C2CC4=CC=C(S(N)(=O)=O)C=C4)C5=NC(C(O)=O)=CS5)=C1)=O)=O)C(C)(C)C)N6[C@H](C(NCC7=CC=C(C=C7)C8=C(C)N=CS8)=O)C[C@@H](O)C6

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 6105

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 122.86 100

制备储备液 for MS 6105

以下数据基于产品分子量 1228.6。 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 0.81 mL 4.07 mL 8.14 mL
5 mM 0.16 mL 0.81 mL 1.63 mL
10 mM 0.08 mL 0.41 mL 0.81 mL
50 mM 0.02 mL 0.08 mL 0.16 mL

Molarity Calculator

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Reconstitution Calculator

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参考文献 for MS 6105

参考文献是支持产品生物活性的出版物。

Sun et al (2023) Discovery of the first lactate dehydrogenase proteolysis targeting chimera degrader for the treatment of pancreatic cancer. J.Med.Chem. 66 596 PMID: 36538511

If you know of a relevant reference for MS 6105, please let us know.

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关键词: MS 6105, MS 6105 supplier, MS6105, lactate, dehydrogenase, LDHA, degrader, degrades, degraders, proteolysis, targeting, chimera, PROTAC, VHL, von, hippel, lindau, E3, ligase, proteosome, Other, Degraders, 8073, 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