G Protein-Coupled Receptor Ligands

CG 428 View larger

CG 428

AT41224

CAS 2412055-93-5

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$151.00

$151.00 per mg

Quantity Discount Table - Order More To Get More Price Discount

QuantitymgUnit Price ($/mg or $/Unit)Final Price
1100 $67.95 Total: $6,795.00
150 $78.52 Total: $3,926.00
125 $92.11 Total: $2,302.75
110 $108.72 Total: $1,087.20
15 $128.35 Total: $641.75

Data sheet

Molecular FormulaC43H43FN10O6
Molecular Weight814.86
CAS Numbers2412055-93-5
Storage Condition0C Short Term, -20C Long Term
SolubilityDMSO
Purity98% by HPLC
SMILES CodeO=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
ReferencesChen L, et al. Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders. J Med Chem. 2020;63[23] 14562-14575.

More info

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.