CG428

• Description:

  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) [1]. (Pink: TRK inhibitor (HY-118271) ; Black: linker (HY-W067489) ; Blue: CRBN Ligand (HY-41547) )

• 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:

  [1]Chen L, et al. Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders. J Med Chem. 2020 Dec 10;63 (23) :14562-14575.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• CAS Number:

  [2412055-93-5]