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Synonyms:
| 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) |
| 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: 270 mg/mL (704.34 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.22 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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