PT2399
Based on 11 publication(s) in Google Scholar
PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo.
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- Purity: 99.96%
- CAS No.: 1672662-14-4
- 화학식: C17H10F5NO4S
- 분자량:419.32
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보관:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PT2399
More- Cancer Discov. 2025 Oct 9. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2025 Jul 1;16(1):5834. [Abstract]
- EMBO J. 2023 Oct 16;42(20):e113743. [Abstract]
- Cell Prolif. 2025 Dec 30:e70160. [Abstract]
- J Biol Eng. 2024 Jan 22;18(1):11. [Abstract]
- FASEB J. 2022 Jul;36(7):e22410. [Abstract]
- Hum Mol Genet. 2023 Aug 7;32(16):2600-2610. [Abstract]
- Blood Red Cells Iron. 2026 Mar 9.
- the Scripps Research Institute. 2025.
- Biomed Pharmacother. 2021 Aug:140:111778. [Abstract]
Biological Activity
IC50: 6 nM (HIF-2α)[3]
PT2399 (compound 10f) inhibits HIF-2α with an IC50 of 6 nM[3].
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PT2399 can bind directly to the HIF-2α PAS B domain, and cripple HIF-2α’s ability to bind to Aryl hydrocarbon receptor nuclear translocator (ARNT)[2].
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PT2399 (20 μM) causes off-target toxicity because it inhibits the proliferation of HIF-2α ?/? 786-O cells and other cancer cell lines with undetectable HIF-2α[2].
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PT2399 (0.2–2 μM; 0-21 days) inhibits 786-O cells soft agar growth[2].
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PT2399 represses various HIF target genes in 786-O VHL?/? ccRCC cells, does not suppress HIF-1α-specific targets such as BNIP3[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:786-O cells
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Concentration:0 μM, 0.2 μM, 2 μM
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Incubation Time:0-21 days
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Result:Inhibited 786-O cell soft agar growth at 0.2–2 μM.
? PT2399 (100 mg/kg; oral gavage; every 12 hours) is more active than SU 11248, and inhibits tumor growth in several SU 11248-resistant tumors in RCC bearing mice [1].
? PT2399 directly inhibits HIF-2α causes tumor regression in preclinical models of primary and metastatic pVHL-defective ccRCC in an on-target fashion[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice with RCC tumorgraft[1]
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Dosage:100 mg/kg
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Administration:Oral gavage; every 12 hours
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Result:More active than SU 11248, and inhibited tumor growth in several SU 11248-resistant tumors.
Chemical Information
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CAS No. 1672662-14-4
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Appearance Solid
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분자량 419.32
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화학식 C17H10F5NO4S
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Color White to off-white
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SMILES
N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C(F)F)=O)C3=C2CC(F)(F)[C@H]3O)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (11)
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Journal Impact Factor
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Most Recent
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Cancer Discov
HIF-2-dependent Regulation of PTHrP and Paraneoplastic Hypercalcemia in Aggressive Clear Cell Renal Cell Carcinoma. [Abstract]2025 Oct 9. PMID: 41065553 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
2025 Jul 1;16(1):5834. PMID: 40595592 -
EMBO J
A mitochondrial EglN1-AMPKα axis drives breast cancer progression by enhancing metabolic adaptation to hypoxic stress. [Abstract]2023 Oct 16;42(20):e113743. PMID: 37661833 -
Cell Prolif
Hypoxia Exacerbates Periapical Periodontitis-Associated Pathological Bone Loss via the Hypoxia-Inducible Factor-2α-Calmodulin-Dependent Protein Kinase IV Axis. [Abstract]2025 Dec 30:e70160. PMID: 41467319 -
J Biol Eng
Poly-3-hydroxybutyrate-co-3-hydroxyvalerate(PHBV)-Polyethylene glycol 20k(PEG20k) as a promising delivery system for PT2399 in the treatment of disc degeneration. [Abstract]2024 Jan 22;18(1):11. PMID: 38254196 -
FASEB J
SGLT2 inhibitor dapagliflozin attenuates cardiac fibrosis and inflammation by reverting the HIF-2α signaling pathway in arrhythmogenic cardiomyopathy. [Abstract]2022 Jul;36(7):e22410. PMID: 35713937 -
Hum Mol Genet
Continuous, but not intermittent, regimens of hypoxia prevent and reverse ataxia in a murine model of Friedreich's ataxia. [Abstract]2023 Aug 7;32(16):2600-2610. PMID: 37260376 -
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Biomed Pharmacother
The HIF-2α/PPARα pathway is essential for liraglutide-alleviated, lipid-induced hepatic steatosis. [Abstract]2021 Aug:140:111778. PMID: 34062416
용액&용해도
DMSO : ≥ 200 mg/mL (476.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (3.98 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (3.98 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Chen W, et al. Targeting renal cell carcinoma with a HIF-2 antagonist. Nature. 2016 Nov 3;539(7627):112-117. [Content Brief]
[2]. Cho H, et al. On-Target Efficacy of a HIF2α Antagonist in Preclinical Kidney Cancer Models. Nature. Nature. 2016 Nov 3;539(7627):107-111. [Content Brief]
[3]. Wehn PM, et al. Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3848 mL | 11.9241 mL | 23.8481 mL | 59.6203 mL |
| 5 mM | 0.4770 mL | 2.3848 mL | 4.7696 mL | 11.9241 mL | |
| 10 mM | 0.2385 mL | 1.1924 mL | 2.3848 mL | 5.9620 mL | |
| 15 mM | 0.1590 mL | 0.7949 mL | 1.5899 mL | 3.9747 mL | |
| 20 mM | 0.1192 mL | 0.5962 mL | 1.1924 mL | 2.9810 mL | |
| 25 mM | 0.0954 mL | 0.4770 mL | 0.9539 mL | 2.3848 mL | |
| 30 mM | 0.0795 mL | 0.3975 mL | 0.7949 mL | 1.9873 mL | |
| 40 mM | 0.0596 mL | 0.2981 mL | 0.5962 mL | 1.4905 mL | |
| 50 mM | 0.0477 mL | 0.2385 mL | 0.4770 mL | 1.1924 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3975 mL | 0.9937 mL | |
| 80 mM | 0.0298 mL | 0.1491 mL | 0.2981 mL | 0.7453 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2385 mL | 0.5962 mL |
PT2399 Related Classifications
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