JBJ-02-112-05

Name: JBJ-02-112-05
Brand: TargetMol
SKU: T11713
Rating: 4.5 (1 reviews)

😃Good

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 IC50 of 15 nM for EGFR L858R/T790M [1].

JBJ-02-112-05

😃Good

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 IC50 of 15 nM for EGFR L858R/T790M [1].

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,520	6-8 weeks	6-8 weeks
50 mg	$1,980	6-8 weeks	6-8 weeks
100 mg	$2,500	6-8 weeks	6-8 weeks

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Resource Download

Product Introduction

Bioactivity

Description	JBJ-02-112-05 is a potent, mutant-selective, allosteric, and orally active inhibitor of EGFR, with an IC50 of 15 nM for EGFR L858R/T790M [1].
Targets&IC50	EGFR (L858R/T790M):15 nM
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 IC50 values of 9.29 μM, 8.35 μM, 8.53 μM, and 2.13 μM, respectively [1]. JBJ-02-112-05 exhibits mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation in Ba/F3 cells stably transfected with EGFR L858R, EGFR L858R/T790M, and 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
Smiles	C(C(NC1=NC=CS1)=O)(N2C(=O)C=3C(C2)=CC=C(C3)C=4C=C5C(=CC4)NC=C5)C6=CC=CC=C6
Relative Density.	1.438 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc