PT-2385

Modify Date: 2024-01-10 04:53:52

PT-2385 Structure
PT-2385 structure
Common Name PT-2385
CAS Number 1672665-49-4 Molecular Weight 383.342
Density 1.6±0.1 g/cm3 Boiling Point 524.7±50.0 °C at 760 mmHg
Molecular Formula C17H12F3NO4S Melting Point N/A
MSDS N/A Flash Point 271.1±30.1 °C

 Use of PT-2385


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

 Names

Name PT2385
Synonym More Synonyms

 PT-2385 Biological Activity

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

 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℃

 Synonyms

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
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