PT-2385 [1672665-49-4]

Cat# NB-64-43013-1mL

Size : 1mLx10mM(inDMSO)

Brand : Neo Biotech

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PT-2385

Catalog No. T7848 Copy Product Info
Purity: 99.55%
PT-2385 is a selective inhibitor of HIF-2α with a dissociation constant (Kd) of less than 50 nM (Kd<50 nM).

PT-2385

Copy Product Info

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

PT-2385
Cas No. 1672665-49-4
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Purity:99.55%
Color:White
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Product Introduction

Bioactivity
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]
Chemical Properties
Molecular Weight383.34
FormulaC17H12F3NO4S
Cas No.1672665-49-4
SmilesCS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12
Relative Density.1.57 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.6087 mL13.0433 mL26.0865 mL130.4325 mL
5 mM0.5217 mL2.6087 mL5.2173 mL26.0865 mL
10 mM0.2609 mL1.3043 mL2.6087 mL13.0433 mL
20 mM0.1304 mL0.6522 mL1.3043 mL6.5216 mL
50 mM0.0522 mL0.2609 mL0.5217 mL2.6087 mL
100 mM0.0261 mL0.1304 mL0.2609 mL1.3043 mL
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.

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