Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
50mg |
|
||
Other Sizes |
|
ln Vitro |
NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3, and PDGFR-β, having IC50 values of 0.38, 0.02 (0.23), 0.18, and 1.4 μM, respectively, according to an enzymatic kinase assay. When the VEGFR-2 inhibitor NVP-ACC789 was added to VEGF-treated cultures, the number of BME cells decreased from 1 μM to baseline values. In a similar vein, NVP-ACC789 markedly inhibited BME cell proliferation caused by bFGF between 1 μM and 10 μM, but not at basal levels. With an IC50 of 1.6 nM, NVP-ACC789 was discovered to be a strong inhibitor of VEGF-induced HUVE cell growth. Additionally, VEGF-induced BME and BAE cell invasion as well as VEGF-C-induced BAE cell invasion were totally prevented by NVP-ACC789. In both cell types, this inhibitory impact was dose-dependent, with peak effects beginning at 1 μM [1].
|
---|---|
ln Vivo |
For six days, NVP-ACC789 is taken orally once a day in a dose-dependent manner to prevent VEGF-induced angiogenesis. To a limited extent, NVP-ACC789 similarly inhibits the bFGF response; however, its dose-response curve is nonlinear [1].
|
References |
[1]. Tille JC, et al. Vascular endothelial growth factor (VEGF) receptor-2 antagonists inhibit VEGF- and basicfibroblast growth factor-induced angiogenesis in vivo and in vitro. J Pharmacol Exp Ther. 2001 Dec;299(3):1073-85
|
Molecular Formula |
C21H17BRN4
|
---|---|
Molecular Weight |
405.29048
|
CAS # |
300842-64-2
|
SMILES |
CC1=C(C=C(C=C1)NC2=NN=C(C3=CC=CC=C32)CC4=CC=NC=C4)Br
|
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) |
DMSO : ~25 mg/mL (~61.68 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4674 mL | 12.3368 mL | 24.6737 mL | |
5 mM | 0.4935 mL | 2.4674 mL | 4.9347 mL | |
10 mM | 0.2467 mL | 1.2337 mL | 2.4674 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.