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.

Safety Information

Hazard Codes 

T

Risk Statements 

25

Safety Statements 

45

RIDADR 

UN 2811 6.1 / PGIII

WGK Germany 

3

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) Scheuermann?et al.?(2013),?Allosteric inhibition of hypoxia inducible factor-2 with small molecules; Nat. Chem. Biol.,?9?271 2) Masetti?et al.?(2014),?Protein dynamics of the HIF-2α PAS-B domain upon heterodimerization and ligand binding; PLoS One,?9(4)?e94986 3) Rodgers?et al.?(2013),?Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor; J. Med. Chem.,?56 1739

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