| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
EGFR-IN-206 (compound 9f) effectively inhibited the proliferation of three EGFR triple mutant cancer cell lines, including Baf3-EGFRL858R/C797S/T790M (IC50 = 33.3 nM), Baf3-EGFRDel19/C797S/T790M (IC50 = 35.8 nM) and H1975-EGFRL858R/C797S/T790M (IC50 = 95.3 nM) [1]. EGFR-IN-206 (10-50 nM, 24 hours) inhibited the migration and invasion of Baf3-EGFRL858R/C797S/T790M cells and H1975-EGFRL858R/C797S/T790M cells [1]. EGFR-IN-206 (50-500 nM) increased the proportion of dead cells in H1975-EGFRL858R/C797S/T790M 3D spheroids in a dose-dependent manner [1]. EGFR-IN-206 (10-1000 nM) decreased the mitochondrial membrane potential of Baf3-EGFRL858R/C797S/T790M and H1975-EGFRL858R/C797S/T790M cells in a dose-dependent manner, promoted apoptosis, and increased intracellular reactive oxygen species levels [1]. EGFR-IN-206 (10-1000 nM) inhibited EGFR phosphorylation in H1975-L858R/C797S/T790M cells in a dose-dependent manner without altering the total EGFR expression level [1]. EGFR-IN-206 inhibited NO secretion in LPS-stimulated Raw264.7 and THP-1 cells, with EC50 values of 101.4 nM and 144.7 nM, respectively [1]. EGFR-IN-206 (10-50 nM; 12 h) significantly reduced IL-6 secretion levels in LPS-stimulated Raw264.7 and THP-1 cells after 12 hours of incubation [1]. EGFR-IN-206 (50-100 nM) inhibited the inflammatory-enhancing colony-forming ability of H1975-L858R/C797S/T790M cells and reduced IL-6 secretion in the THP-1 co-culture model at a concentration of 50 nM [1].
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|---|---|
| ln Vivo |
EGFR-IN-206 (50 mg/kg; orally; once daily for 7 days) achieved a 67.3% tumor growth inhibition rate in nude mice carrying EGFRL858R/T790M/C797S triple mutant H1975 tumors, while reducing the expression levels of p-EGFR and COX-2 in the tumor [1].
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| Cell Assay |
ELISA detection [1]
Cell Types: LPS-stimulated Raw264.7 cells, LPS-stimulated THP-1 cells Tested Concentrations: 10, 50 nM Incubation Duration: 12 hours Experimental Results: Compared with the control group stimulated only by LPS, the secretion of IL-6 in both LPS-stimulated Raw264.7 cells and THP-1 cells was significantly reduced. |
| Animal Protocol |
Animal/Disease Models:Nude Mice [1]
Doses: 50 mg/kg Route of Administration:Oral; once daily; 7 days Experimental Results:Tumor growth inhibition rate (TGI) reached 67.3%. No significant changes in body weight, behavior, or mood were observed. Significantly reduced the expression levels of phosphorylated EGFR (p-EGFR) and COX-2 in tumor tissues. p-EGFR levels were negatively correlated with TGI. COX-2 levels were negatively correlated with TGI. p-EGFR and COX-2 levels were positively correlated. |
| References |
| Molecular Formula |
C32H39N7O4S
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|---|---|
| Molecular Weight |
617.76
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=S(C1CC1)(NC2=CC=CC=C2NC3=C4C=C(OC)C(OC)=CC4=NC(NC5=CC=C(N6CCN(C)CCC6)C(C)=C5)=N3)=O
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6188 mL | 8.0938 mL | 16.1875 mL | |
| 5 mM | 0.3238 mL | 1.6188 mL | 3.2375 mL | |
| 10 mM | 0.1619 mL | 0.8094 mL | 1.6188 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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