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PT-2385

Names

[ CAS No. ]:
1672665-49-4

[ Name ]:
PT-2385

[Synonym ]:
Benzonitrile, 3-[[(1S)-2,2-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro-
3-{[(1S)-2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl]oxy}-5-fluorobenzonitrile
PT-2385

Biological Activity

[Description]:

PT-2385 is a selective HIF-2α antagonist with a Ki of less than 50 nM.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase
Research Areas >> Cancer

[Target]

Kd: <50 nM (HIF-2α)[1]


[In Vitro]

PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α[1].

[In Vivo]

PT-2385 (PT2385) inhibits expression of HIF-2α regulated genes in a dose dependent manner in vivo. Tumor is regressed with PT-2385 (3 and 10 mg/kg, p.o., b.i.d. dose) in 786-O xenograft. PT-2385 (1,3 and 10 mg/kg) also inhibits tumor-derived VEGFA protein levels. PT-2385 (10 mg/kg) treatment reduces proliferation (Ki67) and angiogenesis (CD-31)[1].

[References]

[1]. Eli Wallace, Ph.D. PT2385: HIF-2α Antagonist for the Treatment of VHL Mutant ccRCC. 12th International VHL Medical Symposium April 8, 2016.

[2]. Xie C, et al. Activation of intestinal hypoxia-inducible factor 2α during obesity contributes to hepatic steatosis. Nat Med. 2017 Nov;23(11):1298-1308.


[Related Small Molecules]

Dimethyloxalylglycine | FG-4592 | PX-478 2HCl | BAY 87-2243 | Vadadustat | Daprodustat | Oltipraz | Chlorogenic acid | LW 6 | Molidustat | IOX2 | Paeoniflorin | KC7F2 | oroxylin A | JNJ-42041935

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
524.7±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C17H12F3NO4S

[ Molecular Weight ]:
383.342

[ Flash Point ]:
271.1±30.1 °C

[ Exact Mass ]:
383.043915

[ LogP ]:
1.80

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.613

[ Storage condition ]:
2-8℃

Related Compounds