JBJ-09-063

CAT: 0804-HY-147183Size: 1 EachDry Ice: NoHazardous: No
CAT#:0804-HY-147183Size:1 Each
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Description
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].
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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EGFR/ErbB1/HER1

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Alternative Products

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MF-0138974-01JBJ-09-063
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A24162-50JBJ-09-063 hydrochloride 50mg
A24162-5JBJ-09-063 hydrochloride 5mg
A24162-100JBJ-09-063 hydrochloride 100mg
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