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TL 12-186

Cat. No. 6524 Submit a Review Datasheet / COA / SDS
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Description: Multikinase Degrader (PROTAC®)
Chemical Name: N-(2-(2-(2-(4-(4-((5-Chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)piperazin-1-yl)ethoxy)ethoxy)ethyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)acetamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for TL 12-186

TL 12-186 is a degrader (PROTAC®) comprised of a highly promiscuous kinase inhibitor conjugated to the cereblon E3 ubiquitin ligase ligand, pomalidomide (Cat. No. 6302). Degrades a range of kinases in MOLT-4 and MOLM-14 cell lines.

Negative control TL 13-27 (Cat. No. 6525) is also available.

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

Technical Data for TL 12-186

M. Wt 931.46
Formula C44H51ClN10O9S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2250025-88-6
PubChem ID 134812843
InChI Key YNGWQHGVASHCBK-UHFFFAOYSA-N
Smiles O=C1C(CCC(N1)=O)N2C(C3=C(C2=O)C=CC=C3NCC(NCCOCCOCCN4CCN(CC4)C5=CC=C(C=C5)NC6=NC(NC7=C(C=CC=C7)S(=O)(C(C)C)=O)=C(C=N6)Cl)=O)=O

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 TL 12-186

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 93.15 100

Preparing Stock Solutions for TL 12-186

The following data is based on the product molecular weight 931.46. 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
1 mM 1.07 mL 5.37 mL 10.74 mL
5 mM 0.21 mL 1.07 mL 2.15 mL
10 mM 0.11 mL 0.54 mL 1.07 mL
50 mM 0.02 mL 0.11 mL 0.21 mL

Molarity Calculator

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Reconstitution Calculator

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References for TL 12-186

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

Huang et al (2018) A chemoproteomic approach to query the degradable kinome using a multi-kinase degrader. Cell Chem.Biol. 25 88 PMID: 29129717

If you know of a relevant reference for TL 12-186, please let us know.

View Related Products by Target

Keywords: TL 12-186, TL 12-186 supplier, TL12-186, PROTAC, PROTACs, Proteolysis, targeted, chimeras, cereblon, E3, ubiquitin, ligase, kinase, protein, degradation, tpd, active, degraders, degrades, Other, Kinases, Kinase, Degraders, 6524, Tocris Bioscience

Citations for TL 12-186

Citations are publications that use Tocris products.

Currently there are no citations for TL 12-186. Do you know of a great paper that uses TL 12-186 from Tocris? Please let us know.

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Literature in this Area

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