| Name | PT-2385 |
| Description | PT-2385 is a selective inhibitor of HIF-2α with a dissociation constant (Kd) of less than 50 nM (Kd<50 nM). |
| Animal Research | 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] |
| 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 270 mg/mL (704.34 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.22 mM), Sonication is recommended.
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| Keywords | PT-2385 | PT2385 | PT 2385 | Inhibitor | inhibit | Hypoxia-inducible factors | HIFs | HIFProlylHydroxylase | HIF-PH | HIF-2α | HIF/HIFProlylHydroxylase | HIF/HIF Prolyl-Hydroxylase | HIF/HIF ProlylHydroxylase | HIF Prolyl-Hydroxylase | HIF ProlylHydroxylase | HIF |
| Inhibitors Related | Deferoxamine Mesylate | Hydralazine hydrochloride | Dapagliflozin | Chlorogenic Acid | Glucosamine | Hydroxycitric acid tripotassium hydrate | Glucosamine hydrochloride | Chloramphenicol | Oroxylin A | Acriflavine Hydrochloride | Albendazole | Glucosamine sulfate |
| Related Compound Libraries | Glycolysis Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
