JBJ-09-063 (hydrochloride)

• UNSPSC Description:

  JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer[1].

• Target Antigen:

  EGFR

• Type:

  Reference compound

• Related Pathways:

  JAK/STAT Signaling;Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/jbj-09-063-hydrochloride.html

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  O=C(NC1=NC=CS1)C(C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(C6CCN(C)CC6)C=C5)C=C3)C4=O.[H]Cl

• Molecular Weight:

  593.11

• References & Citations:

  [1]To C, et al. An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. Nat Cancer. 2022 Apr;3(4):402-417.|[2]Gero TW, Scott DA, et al. Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC. Bioorg Med Chem Lett. 2022 Jul 15;68:128718.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  No Development Reported