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PT-2385

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Catalog No. T7848Cas No. 1672665-49-4

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

PT-2385

PT-2385

🥰Excellent
Purity: 99.55%
Catalog No. T7848Cas No. 1672665-49-4
PT-2385 is a selective inhibitor of HIF-2α with a dissociation constant (Kd) of less than 50 nM (Kd<50 nM).
Pack SizePriceAvailabilityQuantity
1 mg$61In Stock
2 mg$89In Stock
5 mg$155In Stock
10 mg$271In Stock
25 mg$433In Stock
50 mg$642In Stock
100 mg$913In Stock
1 mL x 10 mM (in DMSO)$128In Stock
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Purity:99.55%
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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.
Solubility Information
DMSO: 55 mg/mL (143.48 mM)
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

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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