| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Hypoxia-inducible factor 1 alpha (HIF-1α).
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|---|---|
| ln Vitro |
HIF-1α inhibitor-1 is a potent inhibitor of HIF-1α. It inhibits HIF-1α activity in cell-based assays, reducing the expression of HIF-1α target genes involved in angiogenesis (VEGF), metabolism (GLUT1), and survival. Specific IC50 values for HIF-1α inhibition are not detailed in public search results. The compound shows potential as an anticancer agent by targeting the hypoxic tumor microenvironment.
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| ln Vivo |
In vivo efficacy of HIF-1α inhibitor-1 has not been extensively characterized in publicly available literature. As a HIF-1α inhibitor, it would be expected to show antitumor activity in xenograft models by reducing angiogenesis and tumor metabolism. Specific animal model data are limited.
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| Enzyme Assay |
HIF-1α inhibition is assessed using reporter gene assays in cells transfected with a hypoxia-responsive element (HRE)-luciferase construct. Cells are treated with the compound under hypoxic conditions (1% O2) and luciferase activity is measured. HIF-1α protein levels are assessed by Western blot. Target gene expression (VEGF, GLUT1) is measured by qRT-PCR.
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| Cell Assay |
Cellular activity is evaluated in cancer cell lines under hypoxic conditions. Cells are treated with HIF-1α inhibitor-1 at various concentrations and HIF-1α target gene expression is measured. Cell proliferation, migration, and invasion are assessed. VEGF secretion is measured by ELISA. Effects on glycolysis and mitochondrial respiration are evaluated using metabolic assays.
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| Animal Protocol |
In vivo studies for HIF-1α inhibitor-1 are limited. Potential studies could be conducted in mouse xenograft models of cancer. The compound would be administered orally or via intraperitoneal injection. Tumor growth, angiogenesis (CD31 staining), and HIF-1α target gene expression in tumor tissue would be assessed. Specific protocols are not detailed.
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| ADME/Pharmacokinetics |
HIF-1α inhibitor-1 has a molecular formula of C15H11N3O4 and molecular weight of 297.27. The compound is soluble in DMSO. It should be stored at -20°C for up to 3 years or in solvent at -80°C for 1 year. Detailed pharmacokinetic parameters are not extensively characterized.
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| Toxicity/Toxicokinetics |
Safety data for HIF-1α inhibitor-1 indicate it is a research compound for laboratory use only. Specific toxicological profiles including acute toxicity, organ toxicity, and genotoxicity are not extensively published. Standard laboratory safety practices should be followed during handling.
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| References | |
| Additional Infomation |
HIF inhibitor refers to any drug that can inhibit the hypoxia-inducible factor (HIF) subunit.
HIF-1α inhibitor-1 is a research tool compound for studying HIF-1α biology and the hypoxic tumor microenvironment. It is not approved for clinical use. The compound is used to investigate the role of HIF-1α in cancer progression and to validate HIF-1α as a therapeutic target. Its IUPAC name is 2-[[5-(4-cyanophenyl)-3-hydroxypyridine-2-carbonyl]amino]acetic acid. |
| Molecular Formula |
C15H11N3O4
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|---|---|
| Molecular Weight |
297.27
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| Exact Mass |
297.075
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| CAS # |
1000025-14-8
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| PubChem CID |
24891736
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
1.531
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
465
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C#N)C2=CC(=C(N=C2)C(=O)NCC(=O)O)O
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| InChi Key |
FUWDGRQRRUDDDA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11N3O4/c16-6-9-1-3-10(4-2-9)11-5-12(19)14(17-7-11)15(22)18-8-13(20)21/h1-5,7,19H,8H2,(H,18,22)(H,20,21)
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| Chemical Name |
2-[[5-(4-cyanophenyl)-3-hydroxypyridine-2-carbonyl]amino]acetic acid
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| Synonyms |
HIF-1α inhibitor-1; HIF 1α inhibitor 1; HIF1α inhibitor-1
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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 | 3.3639 mL | 16.8197 mL | 33.6395 mL | |
| 5 mM | 0.6728 mL | 3.3639 mL | 6.7279 mL | |
| 10 mM | 0.3364 mL | 1.6820 mL | 3.3639 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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