[CAS NO. 2305154-31-6] JCN037
PRODUCTS SPECIFICATIONS [2305154-31-6]
DESCRIPTION [2305154-31-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 376.18 |
| Molecular Formula | C16H11BrFN3O2 |
| SMILES | FC1=C(Br)C=CC=C1NC2=C3C=C(OCCO4)C4=CC3=NC=N2 |
Summary
IC50 & Target
2.49 nM (EGFR), 3.95 nM (p-wtEGFR), 4.48 nM (pEGFRvⅢ) [1] .
In Vitro
JCN037 exhibits GI 50 values of 329 nM and 1116 nM in HK301 cells and GBM39 cells, respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 664.58 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 6.25 mg/mL (16.61 mM); Clear solution
