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AGN 196996

Names

[ CAS No. ]:
958295-17-5

[ Name ]:
AGN 196996

[Synonym ]:
AGN 196996

Biological Activity

[Description]:

AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM).IC50 value: 2 nM(Ki)Target: RARα antagonistAGN 196996 shows no activity in transactivation assays, but instead block the gene transcriptional activity induced by ATRA and other RAR agonists.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> RAR/RXR
Research Areas >> Cancer

[References]

[1]. Hammond LA, et al. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells. Br J Cancer. 2001 Aug 3;85(3):453-62.

[2]. Keedwell RG, et al. An antagonist of retinoic acid receptors more effectively inhibits growth of human prostate cancer cells than normal prostate epithelium. Br J Cancer. 2004 Aug 2;91(3):580-8.


[Related Small Molecules]

Retinoic acid | AM580 | Tamibarotene | Palovarotene | Fenretinide | TTNPB | Magnolol | AGN 194310 | AGN 193109 | CD437 | Adapalene | AR-7 | Tazarotene | UVI 3003 | Tarenflurbil

Chemical & Physical Properties

[ Density]:
1.453±0.06 g/cm3 (20 °C, 760 mmHg)

[ Boiling Point ]:
619.8±55.0 °C (760 mmHg)

[ Molecular Formula ]:
C24H20BrNO5

[ Molecular Weight ]:
482.32300

[ Exact Mass ]:
481.05200

[ PSA ]:
92.70000

[ LogP ]:
5.41070

[ Storage condition ]:
2-8℃

Related Compounds