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PT2399

Name: PT2399
Brand: TargetMol
SKU: T12675L
Price: 95 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12675L Copy Product Info

Purity: 99.45%

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PT2399 is a potent, selective, orally available HIF-2α antagonist that directly binds to the PAS B domain of HIF-2α (IC₅₀ = 6 nM). PT2399 exhibits antitumor activity. PT2399 specifically blocks the heterodimerization of HIF-2α and HIF-1β, thereby inhibiting the expression of downstream target genes such as VEGF and GLUT1, and exerts its antitumor effects.

Cas No. 1672662-14-4

Pack Size	Price	USA Stock	Global Stock
1 mg	$95	In Stock	In Stock
5 mg	$235	In Stock	In Stock
10 mg	$353	In Stock	In Stock
25 mg	$639	In Stock	In Stock
50 mg	$943	In Stock	In Stock
100 mg	$1,320	-	In Stock
1 mL x 10 mM (in DMSO)	$258	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.45%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	PT2399 is a potent, selective, orally available HIF-2α antagonist that directly binds to the PAS B domain of HIF-2α (IC₅₀ = 6 nM). PT2399 exhibits antitumor activity. PT2399 specifically blocks the heterodimerization of HIF-2α and HIF-1β, thereby inhibiting the expression of downstream target genes such as VEGF and GLUT1, and exerts its antitumor effects.
Targets & IC50	HIF2α:6 nM
In vitro	Methods: HEK293T cells were co-transfected with HIF-2α G323E and HIF-1β F446L expression plasmids. After 36 hours, cells were treated with PT2399 (10 µM) for 5 hours at 37 °C. Immunoprecipitation was performed using anti-FLAG beads (A2220-1ML, Sigma), followed by Western blot analysis. Results: HIF-2α G323E and HIF-1β F446L mutations maintained HIF-2 dimer stability against PT2399-induced dissociation. [1] Methods: RAW 264.7 macrophages were induced to M2 polarization with IL-4/IL-13 (10 ng/mL). Conditioned medium collected after 48 hours of treatment with PT2399 (0.1, 1, 10 μM) in CAFs cultured under 1% O₂ hypoxia was used for 48-hour treatment. RT-qPCR detected Arg1 mRNA levels as an M2 marker. Results: Hypoxic CAF-conditioned medium (CM) significantly enhanced IL-4/13-induced Arg1 expression (promoting M2 polarization). Following PT2399 treatment of CAFs, the pro-M2-polarizing effect of their CM was abolished. [2]
In vivo	Methods: Immunodeficient mice (NOD/SCID) were used to establish a xenograft tumor model. Following successful tumor implantation, oral gavage administration was performed (Sunitinib, 10 mg/kg; PT2399, 100 mg/kg) for 4 consecutive weeks. Results: In sensitive tumors, PT2399 significantly downregulated HIF-2 target gene expression and inhibited tumor cell proliferation and angiogenesis. [1] Methods: C57BL/6 mice were orthotopically inoculated with KPC cells in the pancreas. Following successful inoculation, oral administration of PT2399 (50 mg/kg) was administered twice daily, 5 days per week, for 3 weeks; Intraperitoneal injection of αCTLA4 + αPD1 (dual immune checkpoint blockade, DCB) every 4 days for 2 weeks, with monitoring up to 45 days. Results: The PT2399 + DCB combination therapy group achieved a 100% survival rate at 45 days, significantly higher than the control group and superior to the DCB monotherapy group. [2] Methods: Spinal disc degeneration (APD) model induced by needle puncture in SD rats. PT2399 (10 nmol/kg) administered via local injection through the puncture needle post-surgery; PT2399-PHBV/PP20 (containing equivalent PT2399) administered as a single injection. Animals euthanized at 4, 6, and 8 weeks for tissue collection. Results: In the APD+PT2399-PHBV and APD+PT2399-PP20 groups, histological scores showed a smaller increase and the height/width ratio exhibited a smaller decrease at 6 and 8 weeks, indicating a slowed degeneration process. [3]

Chemical Properties

Molecular Weight	419.32
Formula	C₁₇H₁₀F₅NO₄S
Cas No.	1672662-14-4
Smiles	O[C@H]1c2c(CC1(F)F)c(Oc1cc(F)cc(c1)C#N)ccc2S(=O)(=O)C(F)F
Relative Density.	no data available

Storage & Solubility Information

Storage

Store at low temperature,Store under nitrogen Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 262.5 mg/mL (626.01 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.92 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	2.3848 mL	11.9241 mL	23.8481 mL	119.2407 mL
5 mM	0.4770 mL	2.3848 mL	4.7696 mL	23.8481 mL
10 mM	0.2385 mL	1.1924 mL	2.3848 mL	11.9241 mL
20 mM	0.1192 mL	0.5962 mL	1.1924 mL	5.9620 mL
50 mM	0.0477 mL	0.2385 mL	0.4770 mL	2.3848 mL
100 mM	0.0238 mL	0.1192 mL	0.2385 mL	1.1924 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, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

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 TargetMol | reagent 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 TargetMol | reagent 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 TargetMol | reagent 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.