1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. CNX-2006

CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFRT790M.

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

CNX-2006 Chemical Structure

CNX-2006 Chemical Structure

CAS No. : 1375465-09-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 114 In-stock
Solution
10 mM * 1 mL in DMSO USD 114 In-stock
Solid
1 mg USD 45 In-stock
5 mg USD 95 In-stock
10 mg USD 160 In-stock
50 mg USD 520 In-stock
100 mg USD 950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFRT790M.

IC50 & Target[1]

EGFRT790M

20 nM (IC50)

EGFRL858R/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.
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
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.

  • Molarity Calculator

  • Dilution Calculator

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation
References

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.

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 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.

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Product Name:
CNX-2006
Cat. No.:
HY-13897
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