CG 428

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Description: Potent tropomyosin receptor kinase (TRK) degrader
Chemical Name: 2-(2,6-Dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]-1H-isoindole-1,3(2H)-dione
Purity: ≥98% (HPLC)
Literature (4)

Biological Activity for CG 428

CG 428 is a potent tropomyosin receptor kinase (TRK) Degrader (uSMITETM) (DC50 = 0.36 nM). CG 428 comprises an analog of the pan-TRK inhibitor GNF-8625 joined by a linker to the cereblon E3 ligase ligand pomalidomide (Cat. No. 6302). CG 428 shows selectivity for TRKA over TRKC and TRKB (Kd values = 1nM, 4.2 nM and 28 nM, respectively). Inhibits growth of KM12 colon cancer cells (IC50 =2.9 nM) and is bioavailable.

Negative control CG 428-Neg (Cat. No. 7426), and TrkB antibodies validated for Simple Western™ (automated Western Blot) instruments and Western Blot also available: Catalog # AF1494 and AF397.

Licensing Information

Sold under license from Cullgen

Technical Data for CG 428

E3 ligase CRBN
DC50 0.36 nM (TMP3-TRKA), 2.23 nM (TRKA) - Degradation in KM12/HEL cells after 6 h treatment
Kd (Degrader to Target) 1 nM - Kd was assessed using the KINOMEscan assay
IC50 (Cellular Activity) 2.9 nM - Inhibits growth of KM12 cells
Selectivity confirmed by global proteomics No
M. Wt 814.88
Formula C43H43FN10O6
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2412055-93-5
PubChem ID 146410727
Smiles FC1=CC=CC([C@H]2CCCN2C3=NN4C(C=C3)=NC=C4C5=NC(N6CCN(C(CCOCCNC7=C8C(N(C(C8=CC=C7)=O)C9CCC(NC9=O)=O)=O)=O)CC6)=CC=C5)=C1

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 CG 428

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 81.49 100

Preparing Stock Solutions for CG 428

The following data is based on the product molecular weight 814.88. 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 1.23 mL 6.14 mL 12.27 mL
5 mM 0.25 mL 1.23 mL 2.45 mL
10 mM 0.12 mL 0.61 mL 1.23 mL
50 mM 0.02 mL 0.12 mL 0.25 mL

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References for CG 428

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

Chen et al (2020) Discovery of first-in-class potent and selective tropomyosin receptor kinase degraders. J.Med.Chem. 63 14562 PMID: 33058680

If you know of a relevant reference for CG 428, please let us know.

Keywords: CG 428, CG 428 supplier, CG428, degraders, uSMITE, E3, ligase, TRK, tropomyosin, receptors, kinases, potent, selective, PROTAC, targeted, protein, degradation, Ubiquitin-mediated, Small, Molecule-Induced, Target, Elimination, Active, Degraders, Other, Kinases, 7425, Tocris Bioscience

Citations for CG 428

Citations are publications that use Tocris products.

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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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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