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HIF-2α-IN-2

Cat No.:V41456 Purity: ≥98%
HIF-2α-IN-2 is a hypoxia-inducible factor (HIF-2α) inhibitor (antagonist) with IC50 of 16 nM.
HIF-2α-IN-2
HIF-2α-IN-2 Chemical Structure CAS No.: 1672666-82-8
Product category: New3
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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5mg
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Product Description
HIF-2α-IN-2 is a hypoxia-inducible factor (HIF-2α) inhibitor (antagonist) with IC50 of 16 nM. For more details, check and find compound 232 from the patent WO2015035223A1.
HIF-2α-IN-2 is a selective and potent inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α). It has a molecular weight of 365.35 g/mol and a CAS number of 1672666-82-8. HIF-2α-IN-2 demonstrates an IC50 of 16 nM in a scintillation proximity assay (SPA). It exhibits high binding affinity and selectivity, making it a valuable tool for cancer biology research and the modulation of hypoxic responses.
Biological Activity I Assay Protocols (From Reference)
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.
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.
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.
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.
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.
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.
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.
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.
References

[1]. Aryl ethers and uses thereof. WO2015035223A1.

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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H13F2NO4S
Molecular Weight
365.3512
Exact Mass
365.053
CAS #
1672666-82-8
PubChem CID
117947105
Appearance
White to off-white solid powder
Density
1.52±0.1 g/cm3(Predicted)
Boiling Point
530.6±50.0 °C(Predicted)
LogP
2.1
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
7
Rotatable Bond Count
3
Heavy Atom Count
25
Complexity
643
Defined Atom Stereocenter Count
0
SMILES
CS(=O)(=O)C1=C2C(C(CC2=C(C=C1)OC3=CC(=CC(=C3)C#N)F)F)O
InChi Key
GTHLUQQEKIJSME-UHFFFAOYSA-N
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
Chemical Name
3-fluoro-5-[(2-fluoro-1-hydroxy-7-methylsulfonyl-2,3-dihydro-1H-inden-4-yl)oxy]benzonitrile
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~273.71 mM)
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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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