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CG428

Chemical Structure : CG428

CAS No.: 2412055-93-5

CG428 (CG-428)

Catalog No.: PC-72115Not For Human Use, Lab Use Only.

CG428 (CG-428) is a first-in-class potent and selective TRK degrader (PROTAC) with DC50 of 0.36 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CG428 (CG-428) is a first-in-class potent and selective TRK degrader (PROTAC) with DC50 of 0.36 nM.
CG428 (CG-428) showed selectivity for the degradation of endogenous TPM3-TRKA over ectopically expressed ATP/GTP binding protein-like 4 (AGBL4)-TRKB or ETS variant transcription factor 6 (ETV6)-TRKC fusion proteins in KM12 cells.
CG428 exhibited higher potency for inhibiting growth of KM12 cells with IC50 of 2.9 nM, compared with the parental TRK kinase inhibitor.
CG428 (CG-428) is a valuable chemical tool compound for investigating the in vivo function of TRK fusion during tumorigenesis

Physicochemical Properties

M.Wt 814.879
Formula C43H43FN10O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(2,6-dioxopiperidin-3-yl)-4-((2-(3-(4-(6-(6-((R)-2-(3-fluorophenyl)pyrrolidin-1-yl)imidazo[1,2-b]pyridazin-3-yl)pyridin-2-yl)piperazin-1-yl)-3-oxopropoxy)ethyl)amino)isoindoline-1,3-dione

References

1. Liqun Chen, et al. J Med Chem. 2020 Dec 10;63(23):14562-14575.

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