| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
TC-S 7009 targets hypoxia-inducible factor-2α (HIF-2α), a transcription factor involved in cellular responses to hypoxia. By binding to the HIF-2α PAS-B domain, TC-S 7009 disrupts HIF-2α-ARNT heterodimerization, decreases HIF-2α DNA-binding activity, and suppresses expression of HIF-2α target genes. The compound shows significantly higher affinity for HIF-2α than HIF-1α (Kd >> 5 μM).
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| ln Vitro |
It has been demonstrated that treatment with TC-S 7009 (0-100 μM; 72 hours; HPF cells) inhibits cell growth more in hypoxic than normoxic circumstances [2]. Treatment with TC-S 7009 at a concentration of 50 μM nearly eliminated cell growth.
In vitro, TC-S 7009 is a potent HIF-2α inhibitor with a Kd of 81 nM. It displays >60-fold selectivity for HIF-2α over HIF-1α (Kd >> 5 μM). The compound disrupts HIF-2α heterodimerization, reduces HIF-2α DNA-binding activity, and suppresses HIF-2α target gene expression. |
| ln Vivo |
In vivo, TC-S 7009 has been applied in models of neurological disorders, autoimmune disease, and cancer where aberrant HIF-2α signaling contributes to pathogenesis. By inhibiting HIF-2α, the compound modulates hypoxia-inducible gene expression and has potential therapeutic applications in these diseases.
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| Enzyme Assay |
In vitro receptor binding assays for TC-S 7009 measure its binding affinity to HIF-2α using surface plasmon resonance or fluorescence polarization. A Kd of 81 nM is determined. Functional assays measure the compound's ability to disrupt HIF-2α-ARNT heterodimerization, reduce DNA-binding activity, and suppress target gene expression.
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: HPF cells in lowoxic terms Tested Concentrations: 0-100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Hypoxia-induced NFATc2 nuclear translocation[ 2]. Under normoxic conditions. In vitro cell-based assays for TC-S 7009 use cells with HIF-2α-dependent reporter genes or endogenous HIF-2α target genes. Cells are treated with serial dilutions of the compound, and HIF-2α activity is measured by reporter gene activity or by qPCR of target genes such as VEGF or erythropoietin. Cell viability is assessed in parallel. |
| Animal Protocol |
In vivo animal models for TC-S 7009 include models of neurological disorders, autoimmune disease, and cancer. The compound is administered via appropriate routes, and its effects on disease progression, HIF-2α target gene expression, and tumor growth are evaluated. Pharmacodynamic studies measure HIF-2α inhibition in target tissues.
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| ADME/Pharmacokinetics |
TC-S 7009 has a molecular formula of C12H6ClFN4O3 and a molecular weight of 308.65 g/mol. It is also known as HIF-C2 and has the chemical name N-(3-chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine. The compound has a purity of ≥98% and is stored at room temperature. It is soluble in DMSO at 62 mg/mL.
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| Toxicity/Toxicokinetics |
The toxicity profile of TC-S 7009 is characterized in preclinical safety studies. As a HIF-2α inhibitor, the compound may affect hypoxia responses and angiogenesis. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM and >60-fold selectivity for HIF-2α over HIF-1α. It binds to the HIF-2α PAS-B domain to disrupt HIF-2α-ARNT heterodimerization, decrease HIF-2α DNA-binding, and suppress HIF-2α target gene expression. TC-S 7009 has been applied in models of neurological disorders, autoimmune disease, and cancer and is intended for laboratory research use only.
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| Molecular Formula |
C12H6CLFN4O3
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| Molecular Weight |
308.6534
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| Exact Mass |
308.011
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| CAS # |
1422955-31-4
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| PubChem CID |
70697712
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.263
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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 |
2
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| Heavy Atom Count |
21
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| Complexity |
399
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CDQUJZKBRAFWNG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H6ClFN4O3/c13-6-3-7(14)5-8(4-6)15-10-2-1-9-11(17-21-16-9)12(10)18(19)20/h1-5,15H
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| Chemical Name |
N-(3-chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine
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| Synonyms |
TC-S 7009; TC S 7009; TCS 7009
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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 : ~50 mg/mL (~162.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (6.74 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2399 mL | 16.1996 mL | 32.3992 mL | |
| 5 mM | 0.6480 mL | 3.2399 mL | 6.4798 mL | |
| 10 mM | 0.3240 mL | 1.6200 mL | 3.2399 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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