| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
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| Targets |
HIF-2α-IN-2 targets hypoxia-inducible factor 2 alpha (HIF-2α), a transcription factor that plays a crucial role in the body's response to low oxygen levels (hypoxia). By inhibiting HIF-2α, the compound disrupts the cellular adaptation to hypoxia, which is often exploited by tumors to promote growth and survival.
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| ln Vitro |
In vitro, HIF-2α-IN-2 is a potent inhibitor of HIF-2α with an IC50 of 16 nM in a scintillation proximity assay. It demonstrates high binding affinity and selectivity for HIF-2α. The compound is used in research applications focusing on cancer biology and the modulation of hypoxic responses.
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| ln Vivo |
In vivo activity data for HIF-2α-IN-2 are not extensively detailed in the available sources. As a selective HIF-2α inhibitor, it has potential for studying the role of HIF-2α in tumor growth and survival. Specific in vivo efficacy data in animal models have not been reported.
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| Enzyme Assay |
The in vitro enzyme assay for HIF-2α-IN-2 involves measuring its inhibition of HIF-2α activity. A scintillation proximity assay (SPA) is used, where the compound's ability to displace a labeled ligand from HIF-2α is measured. The IC50 of 16 nM is determined from dose-response curves.
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| Cell Assay |
Cellular assays for HIF-2α-IN-2 are performed using cancer cell lines grown under hypoxic conditions. Cells are treated with the compound at various concentrations. HIF-2α activity is assessed by measuring the expression of HIF-2α target genes using RT-qPCR or by using reporter gene assays.
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| Animal Protocol |
In vivo animal studies for HIF-2α-IN-2 are not detailed in the available sources. The compound is a research tool for studying HIF-2α function. Specific animal models, dosing regimens, and efficacy data have not been reported in the supplier documentation.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for HIF-2α-IN-2 are not available in the provided sources. The compound has a molecular weight of 365.35 g/mol. It is soluble in DMSO. Specific PK parameters such as half-life, bioavailability, and clearance have not been reported.
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| Toxicity/Toxicokinetics |
Toxicity data for HIF-2α-IN-2 are not reported in the available sources. As a research compound, it is not intended for therapeutic use. Specific toxicological profiles have not been characterized.
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| References | |
| Additional Infomation |
HIF-2α-IN-2 is a research compound for studying HIF-2α function in cancer biology and hypoxia. It is a selective and potent HIF-2α inhibitor with an IC50 of 16 nM. The compound is available from commercial suppliers for research purposes only.
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| Molecular Formula |
C17H13F2NO4S
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|---|---|
| Molecular Weight |
365.3512
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| Exact Mass |
365.053
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| CAS # |
1672666-82-8
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| PubChem CID |
117947105
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| Appearance |
White to off-white solid powder
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| Density |
1.52±0.1 g/cm3(Predicted)
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| Boiling Point |
530.6±50.0 °C(Predicted)
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
643
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CS(=O)(=O)C1=C2C(C(CC2=C(C=C1)OC3=CC(=CC(=C3)C#N)F)F)O
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| InChi Key |
GTHLUQQEKIJSME-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H13F2NO4S/c1-25(22,23)15-3-2-14(12-7-13(19)17(21)16(12)15)24-11-5-9(8-20)4-10(18)6-11/h2-6,13,17,21H,7H2,1H3
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| Chemical Name |
3-fluoro-5-[(2-fluoro-1-hydroxy-7-methylsulfonyl-2,3-dihydro-1H-inden-4-yl)oxy]benzonitrile
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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 : ~100 mg/mL (~273.71 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.84 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 | 2.7371 mL | 13.6855 mL | 27.3710 mL | |
| 5 mM | 0.5474 mL | 2.7371 mL | 5.4742 mL | |
| 10 mM | 0.2737 mL | 1.3686 mL | 2.7371 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.