JBJ-09-063

• Target :

  Others|||EGFR

• Related Pathways :

  Others|||Tyrosine Kinase/Adaptors|||Angiogenesis|||JAK/STAT signaling

• Bioactivity :

  JBJ-09-063 is a mutant-selective allosteric inhibitor of the epidermal growth factor receptor (EGFR), with potent inhibitory activity demonstrated by half-maximal inhibitory concentrations (IC50s) of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S. This compound effectively decreases phosphorylation of EGFR, Akt, and ERK1/2, showing efficacy in both EGFR tyrosine kinase inhibitor (TKI) -sensitive and resistant models. JBJ-09-063 holds potential for research into EGFR-mutant lung cancer.

• Smiles :

  C(C(NC1=NC=CS1)=O)(N2C(=O)C=3C(C2)=CC=C(C3)C4=CC=C(C=C4)C5CCN(C)CC5)C6=C(O)C=CC(F)=C6

• Molecular Formula :

  C31H29FN4O3S

• Molecular Weight :

  556.65

• Shipping Conditions :

  Cool pack

• Storage Temperature :

  -20°C

• CAS Number :

  2820336-67-0