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PT-2385

PT-2385
PT-2385 is a selective inhibitor of HIF-2α with a dissociation constant (Kd) of less than 50 nM (Kd<50 nM).
Catalog No. T7848Cas No. 1672665-49-4
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Purity:99.55%
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PT-2385

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).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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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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
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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