CG 428
Tocris Bioscience, part of Bio-Techne | Catalog # 7425
Potent tropomyosin receptor kinase (TRK) Degrader
Key Product Details
Description
Potent tropomyosin receptor kinase (TRK) Degrader
Product Description
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 CullgenProduct Specifications
Molecular Weight
814.88
Formula
C43H43FN10O6
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Chen Discovery of first-in-class potent and selective tropomyosin receptor kinase degraders. J.Med.Chem. 2020 PMID: 33058680
Product Specific Notices for CG 428
For research use only
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