JBJ-09-063

JBJ-09-063 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 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI) -sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer[1].

Product Specifications

CAS Number

[2820336-67-0]

UNSPSC

12352005

Target

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.html

Solubility

DMSO : 120 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

Molecular Formula

C31H29FN4O3S

Molecular Weight

556.65

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.