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PT-2385 is a selective inhibitor of HIF-2α with a dissociation constant (Kd) of less than 50 nM (Kd<50 nM).

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $61 | In Stock | |
| 2 mg | $89 | In Stock | |
| 5 mg | $155 | In Stock | |
| 10 mg | $259 | In Stock | |
| 25 mg | $433 | In Stock | |
| 50 mg | $621 | In Stock | |
| 100 mg | $865 | In Stock | |
| 200 mg | $1,160 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $128 | In Stock |
| Description | PT-2385 is a selective inhibitor of HIF-2α with a dissociation constant (Kd) of less than 50 nM (Kd<50 nM). |
| Targets&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]. |
| 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] |
| Molecular Weight | 383.34 |
| Formula | C17H12F3NO4S |
| Cas No. | 1672665-49-4 |
| Smiles | CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12 |
| Relative Density. | 1.57 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (143.48 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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