CNX-2006

Cat. No.: HY-13897 Purity: 98.42%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

CNX-2006 Chemical Structure

CAS No. : 1375465-09-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 102	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 102	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 45	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 85	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 288	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

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

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.

Molecular Weight

545.53

Formula

C₂₆H₂₇F₄N₇O₂

CAS No.

1375465-09-0

Appearance

Solid

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.42%

Select Batch:

Data Sheet (271 KB) SDS (252 KB)

COA (247 KB) LCMS (100 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

Complete Stock Solution Preparation Table

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

CNX-2006 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CNX-20061375465-09-0CNX2006CNX 2006EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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