Physicochemical Properties
| Molecular Formula | C26H20F5N3O5 |
| Molecular Weight | 549.45 |
| CAS # | 2789629-84-9 |
| 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 | ERK1 ERK2 p38 MAPK |
| ln Vitro | DCZ19931 (1 nM-10 μM; 24 h) has no evident cytotoxicity on human umbilical vein endothelial cells (HUVECs) [1]. DCZ19931 (500 nM; 24 h) suppresses (10 ng/mL; 12 h) VEGFs-induced endothelial cell proliferation, migration, and tube formation [1]. DCZ19931 (500 nM; 24 h) decreases vascular permeability by downregulating ICAM-1 expression [1]. DCZ19931 (500 nM; 24 h) lowers the expression levels of p-ERK1/2, p-p38 and p-JNK in HUVECs [1]. DCZ19931 also showed anti-angiogenic effects in mouse choroidal sprouting experiment [1]. |
| ln Vivo | In a mouse model of oxygen-induced retinopathy (OIR), DCZ19931 (1 μL, 1 μg/μL; intravenous injection; single dosage) prevents ocular neovascularization[1]. In mice model animals with laser-induced choroidal neovascularization (CNV), DCZ19931 (2 μL, 1 μg/μL; intravenous injection; 7 d) suppresses ocular neovascularization without causing tissue toxicity[1]. |
| Cell Assay |
Western Blot Analysis[1] Cell Types: Human umbilical vein endothelial cells (HUVECs) Tested Concentrations: 500 nM; with or without 50 ng/mL VEGF for 30 min Incubation Duration: 24 hrs (hours) Experimental Results: diminished expression of phosphorylated ERK and phosphorylated p38. |
| Animal Protocol |
Animal/Disease Models: Laser-induced choroidal neovascularization (CNV) model in mice[1] Doses: 2 μL, 1 μg/μL Route of Administration: Intravitreal injection; single dose, monitored for 7 d following laser photocoagulation Experimental Results: Did not cause marked histopathological changes in retinal structures. diminished the areas of CNV lesions, demonstrated anti-angiogenic effect in vivo. Animal/Disease Models: Oxygen-induced retinopathy (OIR) model in mice[1] Doses: 1 μL, 1 μg/μL Route of Administration: Intravitreal injection; single dose Experimental Results: Further demonstrated anti-angiogenic effect in vivo, inhibited ocular neovascularization. |
| References |
[1]. DCZ19931, a novel multi-targeting kinase inhibitor, inhibits ocular neovascularization. Sci Rep. 2022 Dec 13;12(1):21539. |
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 | 1.8200 mL | 9.1000 mL | 18.2000 mL | |
| 5 mM | 0.3640 mL | 1.8200 mL | 3.6400 mL | |
| 10 mM | 0.1820 mL | 0.9100 mL | 1.8200 mL |