| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
NVP-QAV-572 targets phosphoinositide 3-kinase (PI3K) enzymes, which are involved in various cellular processes including cell growth, proliferation, and survival. It is a potent inhibitor with an IC₅₀ of 10 nM. By inhibiting PI3K, it modulates signaling pathways involved in inflammation and allergic responses.
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|---|---|
| ln Vitro |
Conditions mediated by Pi3 kinase activation, especially inflammatory or allergic conditions, can be treated with NVP-QAV-572 (Example 8) [1].
In vitro, NVP-QAV-572 demonstrates potent inhibition of PI3K with an IC₅₀ of 10 nM. It is useful for studying PI3K-mediated signaling pathways in inflammatory and allergic conditions. The compound's activity is confirmed in cell-based assays measuring PI3K downstream signaling, such as Akt phosphorylation. |
| ln Vivo |
In vivo, NVP-QAV-572 has been studied for its potential in treating inflammatory and allergic conditions. By inhibiting PI3K, it modulates immune responses and reduces inflammation. It has been investigated in animal models of inflammatory diseases.
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| Enzyme Assay |
The in vitro enzyme assay for NVP-QAV-572 involves measuring the inhibition of PI3K kinase activity. Recombinant PI3K enzymes are incubated with the compound and a substrate such as phosphatidylinositol (4,5)-bisphosphate (PIP2) in the presence of ATP. The production of phosphatidylinositol (3,4,5)-trisphosphate (PIP3) is quantified. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for NVP-QAV-572 are performed using immune cells or other cell lines. Cells are treated with the compound, and PI3K activity is measured by assessing the phosphorylation of downstream targets such as Akt. Cell proliferation, cytokine production, and other functional readouts are also assessed.
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| Animal Protocol |
In vivo animal experiments for NVP-QAV-572 have been conducted in models of inflammatory or allergic diseases. Animals are administered the compound via appropriate routes, and disease severity is assessed. Inflammatory markers, immune cell infiltration, and other pharmacodynamic parameters are measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NVP-QAV-572 have been characterized in preclinical species. It achieves sufficient plasma concentrations to exert its pharmacological effects. Detailed PK parameters such as half-life, clearance, and bioavailability are determined from plasma concentration-time profiles.
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| Toxicity/Toxicokinetics |
Toxicological data for NVP-QAV-572 are limited as it is a research compound. In standard preclinical safety assessments, it would be evaluated for potential off-target effects and general toxicity. The compound is intended for research use only and not for therapeutic use in humans.
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| References | |
| Additional Infomation |
NVP-QAV-572 is a PI3K inhibitor that has been investigated for the treatment of inflammatory and allergic conditions. It is a tool compound for studying PI3K-mediated signaling pathways. It has not been approved for clinical use and remains an investigational research compound.
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| Molecular Formula |
C17H19F2N7O3S2
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|---|---|
| Molecular Weight |
471.504666566849
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| Exact Mass |
471.096
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| CAS # |
957209-68-6
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| PubChem CID |
23581840
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| Appearance |
White to off-white solid powder
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| Density |
1.59±0.1 g/cm3 (20 °C, 760 mmHg)
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| LogP |
3.526
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
714
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(SC(=N1)NC(=O)NCCC2=NN(N=N2)CCF)C3=CC(=C(C=C3)S(=O)(=O)C)F
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| InChi Key |
UGEZRRNNFHAJTM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H19F2N7O3S2/c1-10-15(11-3-4-13(12(19)9-11)31(2,28)29)30-17(21-10)22-16(27)20-7-5-14-23-25-26(24-14)8-6-18/h3-4,9H,5-8H2,1-2H3,(H2,20,21,22,27)
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| Chemical Name |
1-[2-[2-(2-fluoroethyl)tetrazol-5-yl]ethyl]-3-[5-(3-fluoro-4-methylsulfonylphenyl)-4-methyl-1,3-thiazol-2-yl]urea
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| Synonyms |
NVP-QAV-572; NVP QAV-572; NVP-QAV 572; NVP QAV 572; NVP QAV572
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~265.11 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.41 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 20.8 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 | 2.1209 mL | 10.6045 mL | 21.2089 mL | |
| 5 mM | 0.4242 mL | 2.1209 mL | 4.2418 mL | |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1209 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.
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