| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Pichromene targets the PI3K (phosphoinositide 3-kinase) pathway, but it is described as a weak PI3K inhibitor. Its primary anticancer activity may involve additional mechanisms beyond direct PI3K inhibition, possibly including modulation of D-cyclin transactivation.
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|---|---|
| ln Vitro |
A typical in vitro assay for Pichromene involves treating cancer cell lines (e.g., leukemia, myeloma cells) with increasing concentrations of the compound. Cell viability is measured after 48-72 hours using MTT or CellTiter-Glo assays. Mechanistic studies may include analysis of PI3K pathway components (AKT phosphorylation) and cell cycle progression by flow cytometry.
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| ln Vivo |
No detailed in vitro data beyond its classification as a weak PI3K inhibitor and anticancer agent is provided. Pichromene (S14161) has been shown to effectively inhibit tumor growth in leukemia mouse models, indicating robust in vivo antitumor activity despite its weak direct PI3K inhibition.
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| Enzyme Assay |
A typical biochemical PI3K inhibition assay is performed using purified recombinant PI3K enzyme. Increasing concentrations of Pichromene are incubated with the enzyme, ATP, and a PIP2 substrate. The amount of PIP3 produced is measured using a competitive fluorescence polarization or HTRF assay to calculate the IC50, noting that Pichromene is a weak inhibitor.
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| Cell Assay |
For cell-based assays, leukemia and myeloma cell lines (e.g., U266, RPMI-8226) are seeded in 96-well plates. Cells are treated with a concentration range of Pichromene (e.g., 0.1-50 microM) for 48-72 hours. Cell viability is measured using the CellTiter-Glo luminescent assay. Apoptosis may be assessed by Annexin V/PI staining via flow cytometry, and cell cycle distribution is analyzed by propidium iodide staining.
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| Animal Protocol |
The in vivo efficacy of Pichromene (S14161) is evaluated in leukemia mouse models (e.g., xenograft models). Immunodeficient mice are injected subcutaneously or intravenously with human leukemia cells. When tumors are established, mice are treated with Pichromene (e.g., 10-50 mg/kg) via oral gavage or intraperitoneal injection daily or every other day for 2-4 weeks. Tumor volumes are measured with calipers, and survival is monitored.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is reported for Pichromene. Based on its weak PI3K inhibition and in vivo efficacy in leukemia mouse models, Pichromene may have favorable absorption and distribution properties, though specific parameters such as half-life, Cmax, and bioavailability are not provided.
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| Toxicity/Toxicokinetics |
No specific toxicology data is reported for Pichromene. As a weak PI3K inhibitor and anticancer agent with in vivo efficacy in leukemia models, comprehensive toxicological profiling has not been detailed in the provided references.
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| References |
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| Additional Infomation |
An antitumor drug that inhibits the expression of cyclins D1, D2 and D3 and arrests cells in the G0/G1 phase.
Pichromene (S14161; CAS: 883046-50-2) is an anticancer agent and weak PI3K inhibitor. It has molecular formula C17H14FNO4 and molecular weight 315.30. Pichromene can effectively inhibit tumor growth in leukemia mouse models and may be utilized in cancer research. Synonyms: 8-Ethoxy-2-(4-fluorophenyl)-3-nitro-2H-1-benzopyran, 8-Ethoxy-2-(4-fluorophenyl)-3-nitro-2H-chromene. |
| Molecular Formula |
C17H14FNO4
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|---|---|
| Molecular Weight |
315.30
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| Exact Mass |
315.09
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| CAS # |
883046-50-2
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| PubChem CID |
2732983
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
456.2±45.0 °C at 760 mmHg
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| Flash Point |
229.7±28.7 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.613
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
456
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[O-][N+](C1C(C2C=CC(F)=CC=2)OC2C(=CC=CC=2OCC)C=1)=O
|
| InChi Key |
BFZXDHIUPNWOMT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H14FNO4/c1-2-22-15-5-3-4-12-10-14(19(20)21)16(23-17(12)15)11-6-8-13(18)9-7-11/h3-10,16H,2H2,1H3
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| Chemical Name |
8-ethoxy-2-(4-fluorophenyl)-3-nitro-2H-chromene
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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) |
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
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|---|---|
| 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 | 3.1716 mL | 15.8579 mL | 31.7158 mL | |
| 5 mM | 0.6343 mL | 3.1716 mL | 6.3432 mL | |
| 10 mM | 0.3172 mL | 1.5858 mL | 3.1716 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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