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CNX-2006

Catalog No. T6008 CAS 1375465-09-0

Synonyms: CNX 2006, CNX2006

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

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CNX-2006, CAS 1375465-09-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 76.00
10 mg	In stock	$ 128.00
25 mg	In stock	$ 235.00
50 mg	In stock	$ 425.00
1 mL * 10 mM (in DMSO)	In stock	$ 92.00

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Purity: 99.16%

Purity: 98.85%

Biological Description

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Storage & Solubility Information

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.

Synonyms	CNX 2006, CNX2006
Molecular Weight	545.53
Formula	C26H27F4N7O2
CAS No.	1375465-09-0

Storage

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

Solubility Information

DMF: soluble

DMSO: 91 mg/mL(166.8 mM)

References and Literature

1. Ohashi K, et al. 2013

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Inhibitor Library Membrane Protein-targeted Compound Library JAK-STAT Compound Library Anti-Liver Cancer Compound Library Anti-Pancreatic Cancer Compound Library Anti-Lung Cancer Compound Library NO PAINS Compound Library

Related Products

Related compounds with same targets

Olmutinib CP-724714 EGFR-IN-16 Beta-Hydroxyisovalerylshikonin Tyrphostin 23 NSC 228155 EGFR/CDK2-IN-4 SU5204

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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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.

Keywords

CNX-2006 1375465-09-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR CNX 2006 HER1 inhibit Epidermal growth factor receptor ErbB-1 CNX2006 Inhibitor inhibitor

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