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JBJ-02-112-05

Catalog No. T11713Cas No. 2748162-29-8

JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active inhibitor of EGFR with an IC 50 of 15 nM for EGFR L858R/T790M [1].

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Pack Size	Price	Availability
25 mg	$1,520	10-14 weeks
50 mg	$1,980	10-14 weeks
100 mg	$2,500	10-14 weeks

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Product Introduction

Bioactivity

Description	JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active inhibitor of EGFR with an IC 50 of 15 nM for EGFR L858R/T790M [1].
In vitro	In Ba/F3 cells, JBJ-02-112-05 inhibits the activities of wildtype EGFR, EGFR L858R, EGFR L858R/T790M and EGFR L858R/T790M/C797S with IC 50 values of 9.29 μM; 8.35 μM; 8.53 μM and 2.13 μM, respectively [1]. JBJ-02-112-05 shows mutant selectivity through inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation in Ba/F3 cells stably transfected with EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S mutations [1].
In vivo	Administering JBJ-02-112-05 (100 mg/kg; oral gavage; once daily for 3 days) to EGFR L858R/T790M/C797S genetically engineered mice effectively inhibits the phosphorylation of EGFR and downstream signaling pathways [1]. This compound has a moderate half-life of 3 hours and reaches a peak concentration (Cmax) of 13.7 μM after an intravenous (i.v.) dose of 3 mg/kg. Furthermore, a 5 mg/kg oral dosage achieves a prolonged half-life of 16.4 hours with a Cmax of 1.31 μM [1].

Chemical Properties

Molecular Weight	464.54
Formula	C27H20N4O2S
Cas No.	2748162-29-8

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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