TC-S 7009

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Cat.No. 5243 - TC-S 7009 | C12H6ClFN4O3 | CAS No. 1422955-31-4
Description: High affinity and selective HIF-2α inhibitor
Chemical Name: N-(3-Chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

High affinity and selective HIF-2α inhibitor (Kd = 81 nM). Binds to the HIF-2α PAS-B domain; disrupts HIF-2α-ARNT heterodimerization. Exhibits >60-fold selectivity for HIF-2α over HIF-1α. Decreases HIF-2α DNA-binding and attenuates expression of HIF-2α target genes in vitro.

Compound Libraries

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Technical Data

M. Wt 308.65
Formula C12H6ClFN4O3
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 1422955-31-4
PubChem ID 70697712
InChI Key CDQUJZKBRAFWNG-UHFFFAOYSA-N
Smiles ClC1=CC(F)=CC(NC3=C([N+]([O-])=O)C2=NON=C2C=C3)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 30.86 100

Preparing Stock Solutions

The following data is based on the product molecular weight 308.65. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.24 mL 16.2 mL 32.4 mL
5 mM 0.65 mL 3.24 mL 6.48 mL
10 mM 0.32 mL 1.62 mL 3.24 mL
50 mM 0.06 mL 0.32 mL 0.65 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Scheuermann et al (2013) Allosteric inhibition of hypoxia inducible factor-2 with small molecules. Nat.Chem.Biol. 9 271 PMID: 23434853

Rogers et al (2013) Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor. J.Med.Chem. 56 1739 PMID: 23363003


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View all Hypoxia Inducible Factor Inhibitors

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Citations for TC-S 7009

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