2,1,3-Benzoxadiazol-5-aMine, N-(3-chloro-5-fluorophenyl)-4-nitro-
2,1,3-Benzoxadiazol-5-aMine, N-(3-chloro-5-fluorophenyl)-4-nitro- Basic information
- Product Name:
- 2,1,3-Benzoxadiazol-5-aMine, N-(3-chloro-5-fluorophenyl)-4-nitro-
- Synonyms:
-
- 2,1,3-Benzoxadiazol-5-aMine, N-(3-chloro-5-fluorophenyl)-4-nitro-
- HIF-C2
- HIF-2 Antagonist 2
- TC-S 7009
- N-(3-Chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine
- HIF-2 inhibitor 2
- HIF Inhibitor VII - Calbiochem
- N-(3-Chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine
- CAS:
- 1422955-31-4
- MF:
- C12H6ClFN4O3
- MW:
- 308.6524432
- Mol File:
- 1422955-31-4.mol
2,1,3-Benzoxadiazol-5-aMine, N-(3-chloro-5-fluorophenyl)-4-nitro- Chemical Properties
- Boiling point:
- 430.2±55.0 °C(Predicted)
- Density
- 1.652±0.06 g/cm3(Predicted)
- storage temp.
- room temp
- solubility
- DMSO: soluble15mg/mL, clear
- form
- Yellow powder
- pka
- -2.82±0.48(Predicted)
- color
- white to beige
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20°C for up to 1 month.
2,1,3-Benzoxadiazol-5-aMine, N-(3-chloro-5-fluorophenyl)-4-nitro- Usage And Synthesis
Description
HIF-2α-I2 (1422955-31-4) is a potent and selective HIF-2α inhibitor, Kd=81 nM.1?Binds to the HIF-2α PAS-B domain2?and interferes with Hif-2α / ARNT heterodimerization reducing target gene expression in a cellular model1. Highly selective for HIF-2α displaying a >60-fold selectivity over HIF-1α.1,2
Uses
N-(3-Chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine is a HIF-2α inhibitor which inhibits HIF-2α-ARNT heterodimerization by binding to HIF-2α PAS-B domain. It may be used in therapeutic treatment of HIF-2-driven tumors such as renal cell carcinomas.
storage
Store at RT
References
[1] THOMAS H SCHEUERMANN. Allosteric inhibition of hypoxia inducible factor-2 with small molecules[J]. Nature chemical biology, 2013, 9 4: 271-276. DOI:10.1038/nchembio.1185
[2] MATTEO MASETTI Maurizio R Federico Falchi. Protein dynamics of the HIF-2α PAS-B domain upon heterodimerization and ligand binding.[J]. PLoS ONE, 2014: e94986. DOI:10.1371/journal.pone.0094986
[3] JAMIE L. ROGERS. Development of Inhibitors of the PAS-B Domain of the HIF-2α Transcription Factor[J]. Journal of Medicinal Chemistry, 2013, 56 4: 1739-1747. DOI:10.1021/jm301847z
2,1,3-Benzoxadiazol-5-aMine, N-(3-chloro-5-fluorophenyl)-4-nitro-Supplier
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