PT-2385 是一种选择性HIF-2α抑制剂，Ki< 50 nM。

PT-2385 is a selective HIF-2α inhibitor (Kd<50 nM).

PT-2385 is a selective antagonist of HIF-2 and inactive for HIF-1α [1].

PT-2385 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]. PT-2385 (30 or 100 mg/kg; oral gavage; twice daily) result in a rapid, dose-dependent tumor regression [2].

Animal Model: SCID/beige mice with the 786-O and A498 RCC cell lines. Dosage: 30 or 100 mg/kg. Administration: Oral gavage; twice daily [2]

1672665-49-4

C17H12F3NO4S

383.34

DMSO:50 mg/mL (130.43 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years