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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
HIF1-IN-3 targets hypoxia-inducible factor 1 (HIF-1). HIF-1 is a transcription factor that plays a central role in the cellular response to hypoxia, regulating the expression of genes involved in angiogenesis, metabolism, and cell survival. By inhibiting HIF-1 with an EC50 of 0.9 µM, the compound disrupts these adaptive mechanisms, potentially limiting tumor growth and metastasis.
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| ln Vitro |
In vitro, HIF1-IN-3 is a potent inhibitor of HIF-1 with an EC50 of 0.9 µM. It shows inhibitory activity against HIF-1, suggesting its potential in anti-cancer research. However, detailed in vitro activity data against other targets are not extensively reported in the available literature.
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| ln Vivo |
In vivo, HIF1-IN-3 is expected to show efficacy in animal models of cancer by inhibiting HIF-1 activity. However, specific in vivo efficacy data and detailed animal study results are not extensively reported in the available literature. The compound is primarily used as a research tool for studying hypoxia-driven cancers.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for HIF1-IN-3 typically involve cell-based reporter assays to measure HIF-1 transcriptional activity. Cells are transfected with a luciferase reporter gene under the control of a hypoxia response element (HRE). The cells are then treated with the compound under hypoxic conditions, and luciferase activity is measured. The EC50 for HIF-1 inhibition is determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for HIF1-IN-3 are performed using cancer cell lines under hypoxic conditions. Cells are treated with various concentrations of the compound. The expression of HIF-1 target genes (e.g., VEGF, GLUT1) is measured by qPCR or Western blotting. Cell viability and proliferation are assessed using standard assays like MTT.
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| Animal Protocol |
In vivo animal studies with HIF1-IN-3 would typically be conducted in mouse xenograft models of cancer to evaluate its antitumor efficacy. The compound would be administered, and tumor growth, angiogenesis, and expression of HIF-1 target genes would be assessed. However, specific protocols are not detailed in the available literature.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of HIF1-IN-3 are not extensively reported. It has a molecular weight of 412.48. Specific parameters such as oral bioavailability, half-life, and tissue distribution are not detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of HIF1-IN-3 is not extensively reported in the available literature. As a research compound, it is for research use only and not for human therapeutic use. No specific toxicity data are detailed.
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| References | |
| Additional Infomation |
HIF1-IN-3 (compound F4) is a potent inhibitor of HIF-1 with an EC50 of 0.9 µM. It is used in anti-cancer research to study the role of HIF-1 in tumor growth and metastasis. The compound is available for research purposes only.
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| Molecular Formula |
C26H24N2O3
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|---|---|
| Molecular Weight |
412.48
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| Exact Mass |
412.178
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| CAS # |
333314-79-7
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| PubChem CID |
2930221
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
557
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C=CC(CCC(NC(C2C=CC(OC)=CC=2)C2=C(C3N=CC=CC=3C=C2)O)=O)=CC=1
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| InChi Key |
RFCCQJJHFAITGH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H24N2O3/c1-31-21-13-10-20(11-14-21)24(28-23(29)16-9-18-6-3-2-4-7-18)22-15-12-19-8-5-17-27-25(19)26(22)30/h2-8,10-15,17,24,30H,9,16H2,1H3,(H,28,29)
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| Chemical Name |
N-[(8-hydroxyquinolin-7-yl)-(4-methoxyphenyl)methyl]-3-phenylpropanamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~303.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.04 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 20.8 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: ≥ 2.08 mg/mL (5.04 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 | 2.4244 mL | 12.1218 mL | 24.2436 mL | |
| 5 mM | 0.4849 mL | 2.4244 mL | 4.8487 mL | |
| 10 mM | 0.2424 mL | 1.2122 mL | 2.4244 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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