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HER2 PROTAC® CH7C4

Cat. No. 7886 Submit a Review Datasheet / COA / SDS
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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 (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

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)
CAS Number 2897640-93-4
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

Molarity Calculator

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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).

Reconstitution Calculator

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Product Datasheets for HER2 PROTAC® CH7C4

Certificate of Analysis / Product Datasheet
Safety Datasheet

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.

View Related Products by Target

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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.

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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.

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