JBJ-04-125-02 is a mutant-selective allosteric inhibitor of EGFR.

Product information

CAS Number: 2140807-05-0

Molecular Weight: 543.61

Formula: C29H26FN5O3S

Synonym:

(Rac)-JBJ-04-125-02

JBJ-04-125-02 racemate

Chemical Name: 2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxo-6-(4-(piperazin-1-yl)phenyl)isoindolin-2-yl)-N-(thiazol-2-yl)acetamide

Smiles: OC1=CC=C(F)C=C1C(C(=O)NC1=NC=CS1)N1CC2=CC=C(C=C2C1=O)C1C=CC(=CC=1)N1CCNCC1

InChiKey: VHQVOTINPRYDAO-UHFFFAOYSA-N

InChi: InChI=1S/C29H26FN5O3S/c30-21-5-8-25(36)24(16-21)26(27(37)33-29-32-11-14-39-29)35-17-20-2-1-19(15-23(20)28(35)38)18-3-6-22(7-4-18)34-12-9-31-10-13-34/h1-8,11,14-16,26,31,36H,9-10,12-13,17H2,(H,32,33,37)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO 100 mg/mL (183.96 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

JBJ-04-125-02 can inhibit cell proliferation in vitro. Osimertinib, an ATP-competitive covalent EGFR inhibitor, uniquely and significantly enhances the binding of JBJ-04-125-02 for mutant EGFR. The combination of osimertinib and JBJ-04-125-02 results in an increase in apoptosis, a more effective inhibition of cellular growth in vitro compared to either single agent alone.

In Vivo:

JBJ-04-125-02 can inhibit EGFR L858R/T790M/C797S signaling in vivo. The combination of osimertinib and JBJ-04-125-02 results in an increase in apoptosis, and an increased efficacy in vivo compared to either single agent alone.

References:

1. Ciric To, et al. Cancer Discov. 2019 Jul;9(7):926-943.

Products are for research use only. Not for human use.