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HEMTAC 26

Cat. No. 7940 Submit a Review Datasheet / COA / SDS
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Description: CDK6 and CDK4 HSP90-mediated targeting chimera (HEMTAC) Degrader
Chemical Name: 4-[6-[(6-Acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-N-[[1-[4-[2-amino-4-chloro-7-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-3-butyn-1-yl]-1H-1,2,3-triazol-4-yl]methyl]-1-piperazineacetamide
Purity: ≥95% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for HEMTAC 26

HEMTAC 26 is a potent HSP90-mediated targeting chimera (HEMTAC) that degrades CDK6 and CDK4 (DC50 values are 19 nM and 26 nM; Dmax = 92% and 88% in B16F10 cells, 36h treatment). HEMTAC 26 inhibits growth of a range of cancer cell lines including B16F10 and A375 (IC50 values are 112 nM and 126 nM respectively). Induces cell cycle arrest at G0/G1 phase in B16F10 cells.

Technical Data for HEMTAC 26

M. Wt 953.51
Formula C48H53ClN16O4
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 2821803-61-4
PubChem ID 167312304
InChI Key VSAXVERDPZMCPX-UHFFFAOYSA-N
Smiles O=C1C(C(C)=O)=C(C)C2=C(N1C3CCCC3)N=C(NC4=NC=C(N5CCN(CC5)CC(NCC6=CN(CCC#CC7=CN(CC8=NC=C(C)C(OC)=C8C)C9=C7C(Cl)=NC(N)=N9)N=N6)=O)C=C4)N=C2

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 HEMTAC 26

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 95.35 100

Preparing Stock Solutions for HEMTAC 26

The following data is based on the product molecular weight 953.51. 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 1.05 mL 5.24 mL 10.49 mL
5 mM 0.21 mL 1.05 mL 2.1 mL
10 mM 0.1 mL 0.52 mL 1.05 mL
50 mM 0.02 mL 0.1 mL 0.21 mL

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References for HEMTAC 26

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

Li et al (2023) Targeted protein degradation induced by HEMTACs based on HSP90. J.Med.Chem. 66 733 PMID: 36574496

If you know of a relevant reference for HEMTAC 26, please let us know.

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Citations for HEMTAC 26

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Literature in this Area

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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