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SJ 11646

Cat. No. 7721 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 LCK Degrader (PROTAC®)
化学名： N-(2-Chloro-6-methylphenyl)-2-((6-(4-(3-(2-(4-(2,6-dioxopiperidin-3-yl)phenoxy)acetamido)propyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide
纯度： ≥98% (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 SJ 11646

SJ 11646 is a potent LCK (lymphocyte-specific protein tyrosine kinase) Degrader (PROTAC®; DC50 = 0.00838 pM). It comprises Dasatinib (Cat. No. 6793), as the LCK ligand, and a phenyl glutarimide-based cereblon binder. It shows cytotoxicity in LCK-activated T cell acute lymphoblastic leukemia (T-ALL) cell lines and primary leukemia samples in vitro. In vivo, SJ11646 shows anti-leukemic efficacy in patient-derived xenograft models of T-ALL.

LCK antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF3704 and MAB37041.

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

许可信息

Sold under license from St. Jude Children's Research Hospital.

技术数据 for SJ 11646

分子量 746.28
公式 C36H40ClN9O5S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2933135-82-9
InChI Key AJNQGWOQPRWRML-UHFFFAOYSA-N
Smiles CC1=NC(NC2=NC=C(C(NC3=C(C=CC=C3Cl)C)=O)S2)=CC(N4CCN(CC4)CCCNC(COC5=CC=C(C=C5)C6CCC(NC6=O)=O)=O)=N1

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 SJ 11646

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 14.93 20

制备储备液 for SJ 11646

以下数据基于产品分子量 746.28。 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
0.2 mM 6.7 mL 33.5 mL 67 mL
1 mM 1.34 mL 6.7 mL 13.4 mL
2 mM 0.67 mL 3.35 mL 6.7 mL
10 mM 0.13 mL 0.67 mL 1.34 mL

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

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参考文献 for SJ 11646

参考文献是支持产品生物活性的出版物。

Hu et al (2022) Preclinical evaluation of proteolytic targeting of LCK as a therapeutic approach in T cell acute lymphoblastic leukemia. Sci.Transl.Med. 14 eabo5228 PMID: 36001679

If you know of a relevant reference for SJ 11646, please let us know.

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关键词: SJ 11646, SJ 11646 supplier, SJ11646, potent, lymphocyte, specific, kinase, Lck, degraders, degrades, targeted, protein, degradation, TPD, kinases, PROTAC, acute, lymphoblastic, leukemia, T-ALL, Src, Kinases, Kinase, Degraders, 7721, 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