SJ 11646

Pricing Availability   Qty
Description: Potent and selective LCK Degrader (PROTAC®)
Chemical Name: 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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity 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.

Licensing Information

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

Technical Data for SJ 11646

M. Wt 746.28
Formula C36H40ClN9O5S
Storage Store at -20°C
Purity ≥98% (HPLC)
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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for SJ 11646

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 14.93 20

Preparing Stock Solutions for SJ 11646

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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References for SJ 11646

References are publications that support the biological activity of the product.

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.

View Related Products by Target

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Citations for SJ 11646

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Literature in this Area

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Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
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