| Identification | Back Directory | [Name]
PT-2385 | [CAS]
1672665-49-4 | [Synonyms]
CS-2108
PT-2385
PT 2385;PT-2385
Benzonitrile, 3-[[(1S)-2,2-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro- | [Molecular Formula]
C17H12F3NO4S | [MDL Number]
MFCD28963916 | [MOL File]
1672665-49-4.mol | [Molecular Weight]
383.34 |
| Chemical Properties | Back Directory | [Boiling point ]
524.7±50.0 °C(Predicted) | [density ]
1.57±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
DMSO:50.0(Max Conc. mg/mL);130.43(Max Conc. mM) | [form ]
Solid | [pka]
11.28±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
PT2385 is a HIF-2α antagonist with EC50 of 27 nM in the luciferase assay, with no apparent off-target effects. | [in vivo]
PT-2385 (30 or 100 mg/kg; oral gavage; twice daily) result in a rapid, dose-dependent tumor regression[3].
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]. | Animal Model: | SCID/beige mice with the 786-O and A498 RCC cell lines[3] | | Dosage: | 30 or 100 mg/kg | | Administration: | Oral gavage; twice daily | | Result: | Resulted in a rapid, dose-dependent tumor regression.
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| [storage]
Store at -20°C |
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