Cat. No.: HY-13897

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CNX-2006

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CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC₅₀ below 20 nM for EGFR^T790M.

For research use only. We do not sell to patients.

Purity: 98.00%
CAS No.: 1375465-09-0
Formula: C₂₆H₂₇F₄N₇O₂
Molecular Weight:545.53

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CNX-2006 Chemical Structure

CAS No.: 1375465-09-0

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC₅₀ below 20 nM for EGFR^T790M.

IC₅₀ & Target^[1]

EGFR^T790M

20 nM (IC₅₀)

EGFR^L858R/T790M

All EGFR Isoforms :

In Vitro

CNX-2006 inhibits EGFR-T790M cells growth up to 1000-fold more compared to wild-type EGFR cells. EGFR inhibition is observed in cells harbouring the T790M mutation at IC₅₀ values below 20 nM after 1 hour exposure to the drug. CNX-2006 also significantly reduces the volume of tumor spheres derived from H1975 cells^[1]. CNX-2006 exhibits specificity and potent activity against T790M. The drug also shows activity against uncommon EGFR mutations including G719S, L861Q, an exon 19 insertion mutant (I744-K745insKIPVAI), and T854A, but not an exon 20 insertion (H773-V774HVdup). In an in vitro resistance model, CNX-2006 significantly inhibits the emergence of resistant cells. Chronic exposure to escalating doses of CNX-2006 fails to select for and/or enhance T790M-mediated resistance using PC-9 or HCC827 cells (both harboring exon 19 deletions), or PC-9/ER and HCC827/ER cells with existing T790M and resistance to erlotinib^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1375465-09-0
Appearance Solid
Molecular Weight 545.53
Formula C₂₆H₂₇F₄N₇O₂
Color White to gray
SMILES

C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(NC4CN(CCF)C4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 52 mg/mL (95.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8331 mL

9.1654 mL

18.3308 mL

5 mM

0.3666 mL

1.8331 mL

3.6662 mL

10 mM

0.1833 mL

0.9165 mL

1.8331 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Galvani E, et al. Abstract 3244: Role of epithelial-mesenchymal transition (EMT) in sensitivity to CNX-2006, a novel mutant-selective EGFR inhibitor which overcomes in vitro T790M-mediated resistance in NSCLC. CNX-2006, a novel mutant-selective EGFR inhib

[2]. Ohashi K, et al. Abstract 2101A: CNX-2006, a novel irreversible epidermal growth factor receptor (EGFR) inhibitor, selectively inhibits EGFR T790M and fails to induce T790M-mediated resistance in vitro. [abstract]. In: Proceedings of the 104th Annual Meet

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8331 mL	9.1654 mL	18.3308 mL	45.8270 mL
	5 mM	0.3666 mL	1.8331 mL	3.6662 mL	9.1654 mL
	10 mM	0.1833 mL	0.9165 mL	1.8331 mL	4.5827 mL
	15 mM	0.1222 mL	0.6110 mL	1.2221 mL	3.0551 mL
	20 mM	0.0917 mL	0.4583 mL	0.9165 mL	2.2913 mL
	25 mM	0.0733 mL	0.3666 mL	0.7332 mL	1.8331 mL
	30 mM	0.0611 mL	0.3055 mL	0.6110 mL	1.5276 mL
	40 mM	0.0458 mL	0.2291 mL	0.4583 mL	1.1457 mL
	50 mM	0.0367 mL	0.1833 mL	0.3666 mL	0.9165 mL
	60 mM	0.0306 mL	0.1528 mL	0.3055 mL	0.7638 mL
	80 mM	0.0229 mL	0.1146 mL	0.2291 mL	0.5728 mL

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CNX-2006

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All EGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CNX-2006 Related Classifications

Cat. No.: HY-13897