Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PT-2385 is a selective HIF-2α inhibitor (Kd<50 nM).
説明 | PT-2385 is a selective HIF-2α inhibitor (Kd<50 nM). |
ターゲット&IC50 | HIF2α:<50 nM (Kd) |
In vitro | PT-2385 is a selective antagonist of HIF-2 and inactive for HIF-1α [1]. |
In vivo | 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]. |
動物実験 | 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] |
分子量 | 383.34 |
分子式 | C17H12F3NO4S |
CAS No. | 1672665-49-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (143.48 mM)
You can also refer to dose conversion for different animals. 詳細
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PT-2385 1672665-49-4 Angiogenesis Chromatin/Epigenetic Metabolism HIF HIF/HIF Prolyl-Hydroxylase Inhibitor PT2385 inhibit Hypoxia-inducible factors PT 2385 HIF-PH HIFs inhibitor