Biological Activity
CG 428 is a potent tropomyosin receptor kinase (TRK) Degrader (uSMITETM) (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 also available, CG 428-Neg (Cat. No. 7426).
Licensing Information
Sold under license from Cullgen
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Biological Activity
CG 428 is a potent tropomyosin receptor kinase (TRK) Degrader (uSMITETM) (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 also available, CG 428-Neg (Cat. No. 7426).
Licensing Information
Sold under license from Cullgen