| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg | |||
| 50mg | |||
| Other Sizes |
| Targets |
NQO1 substrate targets the enzyme NQO1, serving as its substrate. NQO1 is commonly overexpressed in various cancers, including NSCLC. The compound is designed to be processed by NQO1, potentially leading to cytotoxic effects in cancer cells.
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|---|---|
| ln Vitro |
In cell-free systems, the activity of NQO1 substrate is assessed by its ability to be metabolized by NQO1. This is measured in an enzymatic assay where the compound is incubated with purified NQO1 and NAD(P)H. The conversion of the substrate is quantified. In vitro, NQO1 substrate acts as an efficient NQO1 substrate. It is used in research on NQO1-overexpressing, drug-resistant NSCLC. Its potential antitumor activity is being investigated in cell-based assays.
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| ln Vivo |
In vivo, NQO1 substrate may be a new option for the treatment of NQO1-overexpressing drug-resistant NSCLC. Its in vivo efficacy and safety are likely being evaluated in preclinical models, though specific data is not provided.
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| Enzyme Assay |
The enzymatic activity of NQO1 substrate is measured in a cell-free assay. The compound is incubated with NQO1 and NAD(P)H, and the formation of the product is monitored spectrophotometrically or by HPLC to determine the kinetic parameters.
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| Cell Assay |
Cells, particularly NSCLC cells that overexpress NQO1, are treated with the NQO1 substrate. Cell viability is measured to assess cytotoxicity. The compound's effect on NQO1 activity and downstream signaling is also studied.
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| Animal Protocol |
In vivo efficacy is evaluated in xenograft mouse models of NSCLC. Mice bearing tumors are treated with the compound, and tumor growth is monitored. The compound's ability to inhibit tumor growth and its mechanism of action are studied.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NQO1 substrate are not reported in the provided search results. As a substrate for an intracellular enzyme, its cellular uptake and stability are important factors.
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| Toxicity/Toxicokinetics |
Toxicological data for NQO1 substrate is not available in the provided search results. As a research compound, its safety profile is not well-established. It is intended for research use only.
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| Additional Infomation |
NQO1 substrate is a research tool for studying NQO1 biology and for developing NQO1-dependent anticancer agents. It is a valuable compound for investigating redox biology and cancer metabolism. It is not an approved drug.
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| Molecular Formula |
C13H2F2N4O
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|---|---|
| Molecular Weight |
268.177988529205
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| Exact Mass |
268.019
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| CAS # |
2304503-05-5
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| PubChem CID |
138454764
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
0
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| Heavy Atom Count |
20
|
| Complexity |
535
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=C2C(=CC(=C1F)F)C(=O)C3=NC(=C(N=C23)C#N)C#N
|
| InChi Key |
PZUSGRHVYDQLHR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H2F2N4O/c14-7-1-5-6(2-8(7)15)13(20)12-11(5)18-9(3-16)10(4-17)19-12/h1-2H
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| Chemical Name |
6,7-difluoro-9-oxoindeno[1,2-b]pyrazine-2,3-dicarbonitrile
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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 (~466.10 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (23.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 62.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7288 mL | 18.6442 mL | 37.2884 mL | |
| 5 mM | 0.7458 mL | 3.7288 mL | 7.4577 mL | |
| 10 mM | 0.3729 mL | 1.8644 mL | 3.7288 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.
Products are for research use only; We do not sell to patients
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