Physicochemical Properties
| Molecular Formula | C42H42CLFN4O5 |
| Molecular Weight | 737.26 |
| Appearance | Typically exists as solid at room temperature |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| Targets | EGFR 48.6 nM (IC50) PD-L1 1.77 μM (IC50) |
| ln Vitro | EP26 (0-4 µM; 48 h) reduces the protein expression of p-EGFR in a dose-dependent manner[1]. EP26 (0.5, 1, 2µM; 48 h) induces cell cycle arrest at the G0/G1 phase[1]. EP26 binds to human PD-L1 and mouse PD-L1 in a dose-dependent manner with KD values of 0.58 and 0.52 µM, respectively[1]. |
| ln Vivo | EP26 (50, 100 mg/kg; po; once a day for 21 days) showed antitumor activity in mice [1]. |
| Cell Assay |
Cell Proliferation Assay[1] Cell Types: U87MG, U251, U87MG-vIII, GL261 Tested Concentrations: 0-20 µM Incubation Duration: 72 h Experimental Results: Showed antiproliferative activity with IC50s of 0.77, 1.02, 1.19, 0.28 µM for U87MG, U251, U87MG-vIII, GL261 cells, respectively. Western Blot Analysis[1] Cell Types: U87MG, U87vIII Tested Concentrations: 0, 0.25, 1, 2 µM for U87MG cells, 0, 0.5, 1, 2, 4 µM Incubation Duration: 48 h Experimental Results: Decreased the protein expression of p-EGFR in a dose-dependent manner. Cell Cytotoxicity Assay[1] Cell Types: U87MG Tested Concentrations: 0.5, 1, 2 µM Incubation Duration: 48 h Experimental Results: Induced cell cycle arrest at G0/G1 phase with the percentage of U87MG cells in G0/G1 phase increased from 60.51 to 63.57, 69.48, and 73.98%, respectively. |
| Animal Protocol |
Animal/Disease Models:C57BL/6 mice (GL261 cells)[1] Doses: 50, 100 mg/kg Route of Administration: P.o.; once a day for 21 days Experimental Results: Decreased the tumor weight and tumor volume by 92.0 and 89.7% at 100 mg/kg, significantly inhibited glioblastoma tumor growth with tumor growth inhibitions (TGIs) of 61.4%, 89.4% at 50, 100 mg/kg, respectively. |
| References |
[1]. Discovery of Novel Small-Molecule-Based Potential PD-L1/EGFR Dual Inhibitors with High Druggability for Glioblastoma Immunotherapy. J Med Chem. 2024 May 23;67(10):7995-8019. |
Solubility Data
| 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 |
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3564 mL | 6.7819 mL | 13.5637 mL | |
| 5 mM | 0.2713 mL | 1.3564 mL | 2.7127 mL | |
| 10 mM | 0.1356 mL | 0.6782 mL | 1.3564 mL |