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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)
Biological Activity for CG 428
CG 428 is a potent tropomyosin receptor kinase (TRK) Degrader (uSMITE™) (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) 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 |
| InChI Key | FWANKJAOTQAHHR-KWRHIPAJSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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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Product Datasheets for CG 428
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.
View Related Products by Target
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, Other, Kinases, Raf, and, Ras, Degraders, 7425, Tocris Bioscience
Citations for CG 428
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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 GuideUpdated
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
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- Assays for Protein Degradation
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RAS Oncoproteins Scientific Review
Written by Kirsten L. Bryant, Adrienne D. Cox and Channing J. Der, this review provides a comprehensive overview of RAS protein function and RAS mutations in cancer. Key signaling pathways are highlighted and therapeutic vulnerabilities are explored. This review also includes a detailed section on RAS drug discovery and targeting synthetic lethal interactors of mutant RAS. Compounds available from Tocris are listed.
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