HER2 PROTAC® CH7C4

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Description: Potent and selective HER2 targeting Degrader (PROTAC®)
Chemical Name: 5-((7-(4-(3-((4-((4-([1,2,4]Triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)amino)-6-methoxyquinazolin-7-yl)oxy)propyl)piperazin-1-yl)heptyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity for HER2 PROTAC® CH7C4

HER2 PROTAC® CH7C4 is a potent and selective HER2 (also called ErbB-2) targeting Degrader (PROTAC®) (DC50 = 69 nM; Dmax = 96%). Inhibits BT-474 cell proliferation (IC50 = 47 nM) and xenograft growth. Comprises a Tucatinib (Cat. No. 7640) analog, joined by a linker to a CRBN E3 ligase ligand.

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

Technical Data for HER2 PROTAC® CH7C4

M. Wt 910.05
Formula C49H55N11O7
Storage Store at -20°C
Purity ≥98% (HPLC)
InChI Key IQCKLHMMRZVWLF-UHFFFAOYSA-N
Smiles CC1=C(C=CC(NC2=NC=NC3=CC(OCCCN4CCN(CC4)CCCCCCCNC5=CC(C(N6C7CCC(NC7=O)=O)=O)=C(C=C5)C6=O)=C(C=C32)OC)=C1)OC8=CC9=NC=NN9C=C8

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 HER2 PROTAC® CH7C4

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 91 100

Preparing Stock Solutions for HER2 PROTAC® CH7C4

The following data is based on the product molecular weight 910.05. 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 1.1 mL 5.49 mL 10.99 mL
5 mM 0.22 mL 1.1 mL 2.2 mL
10 mM 0.11 mL 0.55 mL 1.1 mL
50 mM 0.02 mL 0.11 mL 0.22 mL

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Product Datasheets for HER2 PROTAC® CH7C4

References for HER2 PROTAC® CH7C4

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

Hu et al (2022) Discovery of potent and selective HER2 PROTAC degrader based Tucatinib with improved efficacy against HER2 positive cancers. Eur.J.Med.Chem. 244 114775 PMID: 36208507


If you know of a relevant reference for HER2 PROTAC® CH7C4, please let us know.

Keywords: HER2 PROTAC® CH7C4, HER2 PROTAC® CH7C4 supplier, Potent, selective, ErbB2, HER2, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, ErbB, Her, EGFR, Receptor, Tyrosine, Kinases, active, degraders, degrades, PROTAC, PROTACs, targeted, protein, degradation, tpd, Protein, Degraders, 7886, Tocris Bioscience

Citations for HER2 PROTAC® CH7C4

Citations are publications that use Tocris products.

Currently there are no citations for HER2 PROTAC® CH7C4. Do you know of a great paper that uses HER2 PROTAC® CH7C4 from Tocris? Please let us know.

Reviews for HER2 PROTAC® CH7C4

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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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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
Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

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