Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

PT-2385 [1672665-49-4]

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Cat# NB-64-43013-50mg

Size : 50mg

Marca : Neo Biotech

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PT-2385

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Synonyms:

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).

Cas No. 1672665-49-4

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Purity:99.55%

Color:White

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 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 & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.6087 mL	13.0433 mL	26.0865 mL	130.4325 mL
5 mM	0.5217 mL	2.6087 mL	5.2173 mL	26.0865 mL
10 mM	0.2609 mL	1.3043 mL	2.6087 mL	13.0433 mL
20 mM	0.1304 mL	0.6522 mL	1.3043 mL	6.5216 mL
50 mM	0.0522 mL	0.2609 mL	0.5217 mL	2.6087 mL
100 mM	0.0261 mL	0.1304 mL	0.2609 mL	1.3043 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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

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.

Stock Solution Preparation:

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.

Preparation of the In Vivo Formulation:

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.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

PT-2385PT2385PT 2385InhibitorinhibitHypoxia-inducible factorsHIFsHIFProlylHydroxylaseHIF-PHHIF-2αHIF/HIFProlylHydroxylaseHIF/HIF Prolyl-HydroxylaseHIF/HIF ProlylHydroxylaseHIF Prolyl-HydroxylaseHIF ProlylHydroxylaseHIF

Related Tags: PT-2385 chemical structure | PT-2385 in vivo | PT-2385 in vitro | PT-2385 formula | PT-2385 molecular weight