Size | Price | |
---|---|---|
100mg | ||
250mg | ||
500mg | ||
Other Sizes |
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]. Zhang H, et al. DCZ19931, a novel multi-targeting kinase inhibitor, inhibits ocular neovascularization. Sci Rep. 2022 Dec 13;12(1):21539.
|
Molecular Formula |
C26H20F5N3O5
|
---|---|
Molecular Weight |
549.45
|
CAS # |
2789629-84-9
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
O(C1C=CC(=CC=1)C(F)(F)C(=O)NC1C=C(C=C(C=1)C(F)(F)F)OC)C1=NC=NC2C=C(C(=CC=21)OC)OC
|
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)
|
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
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 | 1.8200 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 |
*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.