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CG 428

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Catalog No. T41224Cas No. 2412055-93-5

CG 428 is a potent tropomyosin receptor Kinase (TRK) Degrader (uSMITETM) with a DC50 of 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. CG 428 shows selectivity for TRKA over TRKC and TRKB with Kds of 1nM, 4.2 nM, and 28 nM. CG 428 inhibits the growth of KM12 colon cancer cells with an IC50 of 2.9 nM.

CG 428

CG 428

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Purity: 99.86%
Catalog No. T41224Cas No. 2412055-93-5
CG 428 is a potent tropomyosin receptor Kinase (TRK) Degrader (uSMITETM) with a DC50 of 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. CG 428 shows selectivity for TRKA over TRKC and TRKB with Kds of 1nM, 4.2 nM, and 28 nM. CG 428 inhibits the growth of KM12 colon cancer cells with an IC50 of 2.9 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$178In StockIn Stock
5 mg$445In StockIn Stock
10 mg$656In StockIn Stock
25 mg$987In StockIn Stock
50 mg$1,380In StockIn Stock
100 mg$1,880In StockIn Stock
500 mg$3,780-In Stock
1 mL x 10 mM (in DMSO)$460In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.86%
Appearance:Solid
Color:Yellow
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Product Introduction

CG 428 AI Summary
CG 428 exhibits significant bioactivities, including binding affinity to TRK receptors (TRKA, TRKB, TRKC) and induction of CRBN-mediated TMP3-TRKA protein degradation in human KM12 cells at varying concentrations. It also demonstrates notable antiproliferative activity against human KM12 cells and possesses important pharmacokinetic properties such as Cmax and plasma concentration in ICR mice..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
CG 428 is a potent tropomyosin receptor Kinase (TRK) Degrader (uSMITETM) with a DC50 of 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. CG 428 shows selectivity for TRKA over TRKC and TRKB with Kds of 1nM, 4.2 nM, and 28 nM. CG 428 inhibits the growth of KM12 colon cancer cells with an IC50 of 2.9 nM.
Chemical Properties
Molecular Weight814.86
FormulaC43H43FN10O6
Cas No.2412055-93-5
SmilesO=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2NCCOCCC(=O)N4CCN(CC4)C=5N=C(C=CC5)C=6N7C(=NC6)C=CC(=N7)N8[C@H](CCC8)C9=CC(F)=CC=C9
Relative Density.1.51 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 90 mg/mL (110.45 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.2272 mL6.1360 mL12.2720 mL61.3602 mL
5 mM0.2454 mL1.2272 mL2.4544 mL12.2720 mL
10 mM0.1227 mL0.6136 mL1.2272 mL6.1360 mL
20 mM0.0614 mL0.3068 mL0.6136 mL3.0680 mL
50 mM0.0245 mL0.1227 mL0.2454 mL1.2272 mL
100 mM0.0123 mL0.0614 mL0.1227 mL0.6136 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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