Physicochemical Properties
| Molecular Formula | C23H22N6O4 |
| Molecular Weight | 446.46 |
| Appearance | Typically exists as solids 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 | VEGFR2 0.072 μM (IC50) |
| ln Vitro | VEGFR-2-IN-47 (compound 7g) (48 h) exhibited highly selective antiproliferative activity against MCF-7 and HepG2 cancer cells with IC50 values of 19.35 and 27.89 μM, respectively. VEGFR-2-IN-47 had low toxicity against normal cells (WI-38) with an IC50 value of 51.14 μM, showing good safety[1]. VEGFR-2-IN-47 (19.35 μM; 72 h) caused a decrease in the G0/G1 and S phases of MCF-7 cells and an accumulation in the G2/M phase[1]. VEGFR-2-IN-47 (19.35 μM; 72 h) promoted apoptosis by downregulating the level of Bcl-2 and upregulating the level of Bax in MCF-7 cells, and enhanced immunomodulation by downregulating the level of TNF-α and upregulating the level of IL-2[1]. |
| Cell Assay |
Cell Cycle Analysis[1] Cell Types: MCF-7 Tested Concentrations: 19.35 μM Incubation Duration: 72 hours Experimental Results: Increased the cell population at the G2 / M phase compared to untreated cells from 16.41 to 24.89 %. Induced a decrease in the cell population at the G0 - G1 phase (from 59.04 to 54.51 %) and S phase (from 24.55 to 20.60 %). Apoptosis Analysis[1] Cell Types: MCF-7 Tested Concentrations: 19.35 μM Incubation Duration: 72 hours Experimental Results: Showed a significant increase in early and late apoptosis (17.65 and 7.21 %, respectively) compared to untreated cells (0.43 and 1.71 %, respectively). Real Time qPCR[1] Cell Types: MCF-7 Tested Concentrations: 19.35 μM Incubation Duration: 72 hours Experimental Results: Upregulated the expression of Bax by more than 4.5 times and downregulated Bcl-2 by more than 6 times. Exhibited a strong suppressive effect on the TNF-a (2.5 fold) and stimulatory effect on the IL-2 (3.3 fold) compared to the control cells. |
| References |
[1]. Jingyi Liu, et al. Identification of 3-(9H-carbazol-9-yl)-2-(1,3-dioxoisoindolin-2-yl)propanoic acids as promising DNMT1 inhibitors. Eur J Med Chem. 2024 Aug 5;274:116538. |
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 | 2.2398 mL | 11.1992 mL | 22.3984 mL | |
| 5 mM | 0.4480 mL | 2.2398 mL | 4.4797 mL | |
| 10 mM | 0.2240 mL | 1.1199 mL | 2.2398 mL |