CG428
CG428 is a potent and selective tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 (TPM3) -TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). In addition, CG428 effectively inhibits KM12 cell growth (IC50 = 2.9 nM). (Pink: TRK inhibitor ; Black: linker (HY-W067489) ; Blue: CRBN Ligand (HY-41547) )
Product Specifications
CAS Number
2412055-93-5
UNSPSC
12352005
Target
PROTACs; Trk Receptor
Type
Reference compound
Related Pathways
Neuronal Signaling; PROTAC; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/cg428.html
Purity
98.26
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCC(N4CCN(C5=NC(C6=CN=C7C=CC(N8[C@@H](C9=CC=CC(F)=C9)CCC8)=NN76)=CC=C5)CC4)=O)=O
Molecular Formula
C43H43FN10O6
Molecular Weight
814.86
References & Citations
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Available Sizes
Frequently Asked Questions
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