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CG 428

Catalog #: 7425 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7425/5
CG 428 | CAS No. 2412055-93-5 | Active Degraders
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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%

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Biological Activity

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 (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 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.

Technical Data

E3 ligase
CRBN
DC50
0.36 nM (TMP3-TRKA), 2.23 nM (TRKA) - Degradation in KM12/HEL cells after 6 h treatment
Kd (Degrader to Target)
1 nM - Kd was assessed using the KINOMEscan assay
IC50 (Cellular Activity)
2.9 nM - Inhibits growth of KM12 cells
Selectivity confirmed by global proteomics
No
M.Wt:
814.88
Formula:
C43H43FN10O6
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2412055-93-5

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.

Additional Information

Licensing Caveats:
Sold under license from Cullgen

Product Datasheets

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