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CNX-2006

CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.

Catalog No. T6008Cas No. 1375465-09-0

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Purity:99.16%

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COA HNMR HPLC

CNX-2006

Catalog No. T6008Cas No. 1375465-09-0

CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.

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.

Pack Size	Price	Availability
1 mg	$34	In Stock
2 mg	$48	In Stock
5 mg	$76	In Stock
10 mg	$128	In Stock
25 mg	$235	In Stock
50 mg	$425	In Stock
1 mL x 10 mM (in DMSO)	$92	In Stock

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Product Introduction

Bioactivity

Description	CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
Targets&IC50	EGFR (mutant):<20 nM
In vitro	CNX-2006 is a novel irreversible EGFR tyrosine kinase inhibitor, specifically inhibits activating mutations of EGFR as well as the T790M mutation while having very weak inhibition at wild-type EGFR. In in vitro modeling of acquired resistance, continuous CNX-2006 treatment on drug-sensitive EGFR mutant cells leads to resistance more slowly than erlotinib. Dose escalation with CNX-2006 leads to differential effects in different lines, but does not select for T790M-mediated resistance. [1]CNX-2006 resistent cells shows increased expression of EMT markers and MMP9.[2]
In vivo	CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model. [1] [2]
Kinase Assay	Growth inhibition assays: Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays.
Cell Research	Cells with endogenous or transiently transfected mutant EGFRs (293 cells) are treated with inhibitors for 6 hours and then corresponding lysates are extracted and analyzed by immunoblotting.(Only for Reference)
Animal Research	Animal Models: Nude miceFormulation: 5% DMSO:15% Solutol HS15 in PBSDosages: 25 mg/kgAdministration: i.p.
Alias	CNX 2006, CNX2006

Chemical Properties

Molecular Weight	545.53
Formula	C₂₆H₂₇F₄N₇O₂
Cas No.	1375465-09-0

Storage & Solubility Information

Storage

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

Solubility Information

DMF: soluble

DMSO: 91 mg/mL (166.8 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8331 mL	9.1654 mL	18.3308 mL	91.6540 mL
5 mM	0.3666 mL	1.8331 mL	3.6662 mL	18.3308 mL
10 mM	0.1833 mL	0.9165 mL	1.8331 mL	9.1654 mL
20 mM	0.0917 mL	0.4583 mL	0.9165 mL	4.5827 mL
50 mM	0.0367 mL	0.1833 mL	0.3666 mL	1.8331 mL
100 mM	0.0183 mL	0.0917 mL	0.1833 mL	0.9165 mL

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In Vivo Formulation Calculator (Clear solution)

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

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

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

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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