1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. JCN037

JCN037 (Synonyms: JGK037)

Cat. No.: HY-136430
Handling Instructions

JCN037 (JGK037) is potent, non-covalent and brain-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively.

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

JCN037 Chemical Structure

JCN037 Chemical Structure

CAS No. : 2305154-31-6

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

JCN037 (JGK037) is potent, non-covalent and brain-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively[1].

IC50 & Target

2.49 nM (EGFR), 3.95 nM (p-wtEGFR), 4.48 nM (pEGFRvⅢ)[1].

In Vitro

JCN037 exhibits GI50 values of 329 nM and 1116 nM in HK301 cells and GBM39 cells, respectively[1].

Western Blot Analysis[1].

Cell Line: GBM39 and GS025 cells.
Concentration: 0-3333 nM
Incubation Time:
Result: Downregulated pEGFRvⅢ, p Akt, p-ERK, and p-S6 protein levels, significantly.
In Vivo

JCN037 (compound 5) exhibits low oral bioavailability due to a rapid hydroxylation of the fused 1,4-dioxane ring, suggesting first pass metabolism[1].
JCN037 (compound 5, 300 mg/kg, BID) treatment provides a significant survival benefit, whereby median survival increased by 47% from 37.5 days to 55 days with 5 treatment[1].

Molecular Weight

376.18

Formula

C₁₆H₁₁BrFN₃O₂

CAS No.

2305154-31-6

SMILES

FC1=C(Br)C=CC=C1NC2=C3C=C(OCCO4)C4=CC3=NC=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (664.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6583 mL 13.2915 mL 26.5830 mL
5 mM 0.5317 mL 2.6583 mL 5.3166 mL
10 mM 0.2658 mL 1.3292 mL 2.6583 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6.25 mg/mL (16.61 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

JCN037JGK037JCN 037JCN-037JGK 037JGK-037EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Product name:
JCN037
Cat. No.:
HY-136430
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