CG 428

Name: CG 428
Brand: Tocris Bioscience
SKU: 7425

Tocris Bioscience, part of Bio-Techne | Catalog # 7425

COA / SDS

Potent tropomyosin receptor kinase (TRK) Degrader

Key Product Details

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)
Molecular Weight:	814.88

View Full Technical Details for CG 428

Technical Data
Citations

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 (K_d 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

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
E3 ligase	CRBN
DC₅₀	0.36 nM (TMP3-TRKA), 2.23 nM (TRKA) - Degradation in KM12/HEL cells after 6 h treatment
K_d (Degrader to Target)	1 nM - K_d was assessed using the KINOMEscan assay
IC₅₀ (Cellular Activity)	2.9 nM - Inhibits growth of KM12 cells
Selectivity confirmed by global proteomics	No

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 for CG 428

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for CG 428

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