Cat. No.: HY-12867

PT-2385

Name: PT-2385
Brand: MedChemExpress
SKU: HY-12867
Price: 110.00 USD
Availability: InStock
Rating: 5 (56 reviews)

56 Cited Publications

Customer Review

Based on 56 publication(s) in Google Scholar

PT-2385 is a selective HIF-2α inhibitor with a K_i of less than 50 nM.

For research use only. We do not sell to patients.

Purity : 99.95%
CAS No.: 1672665-49-4
Formula: C₁₇H₁₂F₃NO₄S
Molecular Weight:383.34

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PT-2385 Chemical Structure

CAS No.: 1672665-49-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (56)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PT-2385 is a selective HIF-2α inhibitor with a K_i of less than 50 nM^[1]^[2].

IC₅₀ & Target

Kd: <50 nM (HIF-2α)^[1]

All HIF/HIF Prolyl-Hydroxylase Isoforms :

In Vitro

PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PT-2385 (30 or 100 mg/kg; oral gavage; twice daily) result in a rapid, dose-dependent tumor regression^[3].
PT-2385 (PT2385) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

SCID/beige mice with the 786-O and A498 RCC cell lines^[3]
Dosage:

30 or 100 mg/kg
Administration:

Oral gavage; twice daily
Result:

Resulted in a rapid, dose-dependent tumor regression.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1672665-49-4
Appearance Solid
Molecular Weight 383.34
Formula C₁₇H₁₂F₃NO₄S
Color White to off-white
SMILES

N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C)=O)C3=C2CC(F)(F)[C@H]3O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (56)

All Cell Imaging/StainingWB

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Journal Impact Factor

Nat Med

Activation of intestinal hypoxia-inducible factor 2α during obesity contributes to hepatic steatosis. [Abstract]

2017 Nov;23(11):1298-1308. PMID: 29035368

PT-2385 purchased from MedChemExpress. Usage Cited in: Nat Med. 2017 Nov;23(11):1298-1308. [Abstract]

Western blot analysis of NEU3 protein expression in the small intestine.
Cell Metab

Microbial Metabolite Signaling Is Required for Systemic Iron Homeostasis. [Abstract]

2020 Jan 7;31(1):115-130.e6. PMID: 31708445
Cell Host Microbe

Candida albicans accelerates atherosclerosis by activating intestinal hypoxia-inducible factor2α signaling. [Abstract]

2024 Jun 12;32(6):964-979.e7. PMID: 38754418
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

Chronic cerebral hypoperfusion induces venous dysfunction via EPAS1 regulation in mice. [Abstract]

2025 Jul 8;16(1):6302. PMID: 40628749
Nat Commun

Adipocyte deletion of the oxygen-sensor PHD2 sustains elevated energy expenditure at thermoneutrality. [Abstract]

2024 Aug 29;15(1):7483. PMID: 39209825
Nat Commun

HIF-2α is indispensable for regulatory T cell function. [Abstract]

2020 Oct 6;11(1):5005. PMID: 33024109

PT-2385 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Oct 6;11(1):5005. [Abstract]

WT naïve CD4+ T cells are activated by CD3/CD28 (2/1 μg/mL) in the presence of HIF-2α inhibitor PT2385 for 2 days, or activating WT iTreg cells are treated with 10 μM PT2385, and HIF-1α levels determined. Treatment of activating WT CD4+ T cells with PT2385 leads to dose-dependent upregulation of HIF-1α. PT2385 also increases the level of HIF-1α induction in activated WT iTreg cells.
Mol Cell

2026 Aug 20;86(16):3223-3239.e11. PMID: 42480523
J Clin Invest

Marked and rapid effects of pharmacological HIF-2α antagonism on hypoxic ventilatory control. [Abstract]

2020 May 1;130(5):2237-2251. PMID: 31999648
J Clin Invest

Hepatic hepcidin/intestinal HIF-2α axis maintains iron absorption during iron deficiency and overload. [Abstract]

2019 Jan 2;129(1):336-348. PMID: 30352047
Adv Sci (Weinh)

Lysosome-Featured Cell Aggregate-Released Extracellular Vesicles Regulate Iron Homeostasis and Alleviate Post-Irradiation Endothelial Ferroptosis for Mandibular Regeneration. [Abstract]

2025 Sep;12(34):e05070. PMID: 40546115

PT-2385 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep;12(34):e05070. [Abstract]

Bright-field images for the process of cell aggregation. The results showed that Ferrozine (6.5 mM) slowed the CA formation. Scale bars, 150 µm.
Sci Adv

PAI-1 is a vascular cell-specific HIF-2-dependent angiogenic factor that promotes retinal neovascularization in diabetic patients. [Abstract]

2022 Mar 4;8(9):eabm1896. PMID: 35235351
Biomaterials

HIF-2α-targeted interventional chemoembolization multifunctional microspheres for effective elimination of hepatocellular carcinoma. [Abstract]

2022 May;284:121512. PMID: 35405577
Cell Death Dis

Increasing AR by HIF-2α inhibitor (PT-2385) overcomes the side-effects of sorafenib by suppressing hepatocellular carcinoma invasion via alteration of pSTAT3, pAKT and pERK signals. [Abstract]

2017 Oct 12;8(10):e3095. PMID: 29022906

PT-2385 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2017 Oct 12;8(10):e3095. [Abstract]

Western blot assays show PT-2385 can suppress HIF-2α level and partly reverse the decrease of AR and the increase of downstream signals (pSTAT3, pAKT and pERK) by Bay 43-9006 treatment.
J Hazard Mater

In vitro and in vivo investigations on arsenic-induced cartilage degeneration in osteoarthritis. [Abstract]

2024 Jan 5:461:132570. PMID: 37742380
Proc Natl Acad Sci U S A

Iron regulatory protein 2 contributes to antimicrobial immunity by preserving lysosomal function in macrophages. [Abstract]

2024 Jul 30;121(31):e2321929121. PMID: 39047035
Proc Natl Acad Sci U S A

Essential role of systemic iron mobilization and redistribution for adaptive thermogenesis through HIF2-α/hepcidin axis. [Abstract]

2021 Oct 5;118(40):e2109186118. PMID: 34593646
Arterioscler Thromb Vasc Biol

Low Wall Shear Stress Promotes Atheroma via Arterial Iron Accumulation. [Abstract]

2025 Nov;45(11):1983-1996. PMID: 41036559
Antioxidants (Basel)

Stimulation of Hepatic Ferritinophagy Mitigates Irp2 Depletion-Induced Anemia. [Abstract]

2023 Feb 24;12(3):566. PMID: 36978814
Cell Mol Gastroenterol Hepatol

Intestinal HIF-2α Regulates GLP-1 Secretion via Lipid Sensing in L-Cells. [Abstract]

2022;13(4):1057-1072. PMID: 34902628
Cell Rep

Conserved patterns of transcriptional dysregulation, heterogeneity, and cell states in clear cell kidney cancer. [Abstract]

2025 Jan 8;44(1):115169. PMID: 39792555
Cell Rep

Hypoxia drives HIF2-dependent reversible macrophage cell cycle entry. [Abstract]

2024 Jul 23;43(7):114471. PMID: 38996069
Br J Pharmacol

Established pulmonary hypertension in rats was reversed by a combination of a HIF-2α antagonist and a p53 agonist. [Abstract]

2022 Mar;179(5):1065-1081. PMID: 34599843
Biochem Pharmacol

The 'ABC' of split-nanoluciferase HIF heterodimerization bioassays: Applications, Benefits & Considerations. [Abstract]

2024 Nov:229:116478. PMID: 39128589
Mol Metab

Microbial metabolite deoxycholic acid-mediated ferroptosis exacerbates high-fat diet-induced colonic inflammation. [Abstract]

2024 Jun:84:101944. PMID: 38642891
Int J Pharm

A pH-responsive novel delivery system utilizing carbon quantum dots loaded with PT2385 for targeted inhibition of HIF-2α in the treatment of osteoarthritis. [Abstract]

2024 Dec 5:666:124752. PMID: 39321898
Cancer Immunol Immunother

VHL restoration in clear cell renal cell carcinoma improves NK cell infiltration and function. [Abstract]

2025 Jul 30;74(9):278. PMID: 40736709
Cancer Immunol Immunother

Tumor infiltrating mast cells determine oncogenic HIF-2α-conferred immune evasion in clear cell renal cell carcinoma. [Abstract]

2019 May;68(5):731-741. PMID: 30758643
Int J Mol Sci

Role of Hypoxia-Inducible Factors in Respiratory Syncytial Virus Infection-Associated Lung Disease. [Abstract]

2025 Mar 29;26(7):3182. PMID: 40244000
J Enzyme Inhib Med Chem

Identification of novel HIF2α inhibitors: a structure-based virtual screening approach. [Abstract]

2026 Dec;41(1):2606435. PMID: 41493169
Sci Rep

Characterisation of an autochthonous mouse ccRCC model of immune checkpoint inhibitor therapy resistance. [Abstract]

2025 Jun 5;15(1):19818. PMID: 40473819
Neoplasia

Niche-derived soluble DLK1 promotes glioma growth. [Abstract]

2020 Dec;22(12):689-701. PMID: 33142235
Cell Signal

EP300 promotes renal tubular epithelial cell fibrosis by increasing HIF2α expression in diabetic nephropathy. [Abstract]

2022 Oct:98:110407. PMID: 35839978
Biomedicines

High-Altitude Hypoxia Induces Excessive Erythrocytosis in Mice via Upregulation of the Intestinal HIF2a/Iron-Metabolism Pathway. [Abstract]

2023 Nov 7;11(11):2992. PMID: 38001992
Membranes

Effective Perturbations of the Amplitude, Gating, and Hysteresis of IK(DR) Caused by PT-2385, an HIF-2α Inhibitor. [Abstract]

2021 Aug 17;11(8):636. PMID: 34436399
Curr Issues Mol Biol

IL-1β/EPAS1-Associated Ferroptotic Stress Impairs Skeletal Stem/Progenitor Cell Function in Inflammation-Associated Fracture Nonunion. [Abstract]

2026 Jun 9;48(6):606. PMID: 42353610
J Immunol

Ischemia-free liver transplantation alleviates liver transplant injury caused by CD69+CD103-CD8+T cells by regulating HIF-2α expression. [Abstract]

2026 Apr 15;215(4):vkag005. PMID: 42015528
Drug Metab Dispos

Metabolic Profiling of the Novel Hypoxia-Inducible Factor 2 α Inhibitor PT2385 In Vivo and In Vitro. [Abstract]

2018 Apr;46(4):336-345. PMID: 29363499
Front Oncol

HIF-2α regulates proliferation, invasion, and metastasis of hepatocellular carcinoma cells via VEGF/Notch1 signaling axis after insufficient radiofrequency ablation. [Abstract]

2022 Sep 23;12:998295. PMID: 36212390
Life Sci Alliance

Multi-level interaction between HIF and AHR transcriptional pathways in kidney carcinoma. [Abstract]

2023 Feb 1;6(4):e202201756. PMID: 36725335
Mol Pharmacol

Structural basis for the allosteric inhibition of hypoxia-inducible factor (HIF)-2 by belzutifan. [Abstract]

2022 Sep 27;102(6):MOLPHARM-AR-2022-000525. PMID: 36167425
Mol Cell Biol

Erythropoietin Production in Embryonic Neural Cells is Controlled by Hypoxia Signaling and Histone Deacetylases with an Undifferentiated Cellular State. [Abstract]

2025 Jan;45(1):32-45. PMID: 39620278
PLoS One

A paradoxical method to enhance compensatory lung growth: Utilizing a VEGF inhibitor. [Abstract]

2018 Dec 19;13(12):e0208579. PMID: 30566445
Drug Test Anal

Metabolic study of hypoxia-inducible factor stabilizers BAY 87-2243, MK-8617, and PT-2385 in equine liver microsomes for doping control. [Abstract]

2022 Oct;14(10):1703-1723. PMID: 35853151
Biochem Biophys Res Commun

EPAS1/HIF2α correlates with features of low-risk neuroblastoma and with adrenal chromaffin cell differentiation during sympathoadrenal development. [Abstract]

2019 Jan 22;508(4):1233-1239. PMID: 30563765

PT-2385 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2019 Jan 22;508(4):1233-1239. [Abstract]

Western blot with HIF2a-specific antibody on lysates from LAN-1 cells treated grown in normoxia (21% O₂) or in hypoxia (1% O₂), with the indicated concentration of PT2385.
bioRxiv

Epigenetic de-repression of basal cell metaplasia in aging AT2 cells is a risk factor for idiopathic pulmonary fibrosis (IPF). [Abstract]

2026 Jun 10:2026.06.09.731212. PMID: 42327275
University of California, Irvine

2024.
bioRxiv

2024 August 27.
bioRxiv

HIF2α-dependent inhibition of mitochondrial clustering of glutaminase suppresses clear cell renal cell carcinoma. [Abstract]

2024 May 5:2024.05.04.592520. PMID: 38746132
Environ Toxicol

Roxadustat ameliorates vascular calcification in CKD rats by regulating HIF-2α/HIF-1α. [Abstract]

2024 Apr;39(4):2363-2373. PMID: 38156404
UNIVERSITY OF THESSALY

2023 Sep.
bioRxiv

2023 Sep 17.
Research Square Preprint

2022 Jul.
Research Square Print

2022 Jun.
Biomed Pharmacother

Berberine reduces hepatic ceramide levels to improve insulin resistance in HFD-fed mice by inhibiting HIF-2α. [Abstract]

2022 Jun:150:112955. PMID: 35429745
University of Michigan

2020 Feb.

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (130.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6087 mL

13.0433 mL

26.0865 mL

5 mM

0.5217 mL

2.6087 mL

5.2173 mL

10 mM

0.2609 mL

1.3043 mL

2.6087 mL

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 2.87 mg/mL (7.49 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Eli Wallace, Ph.D. PT2385: HIF-2α Antagonist for the Treatment of VHL Mutant ccRCC. 12th International VHL Medical Symposium April 8, 2016.

[2]. Xie C, et al. Activation of intestinal hypoxia-inducible factor 2α during obesity contributes to hepatic steatosis. Nat Med. 2017 Nov;23(11):1298-1308. [Content Brief]

[3]. Wallace EM, et al. A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma. Cancer Res. 2016 Sep 15;76(18):5491-500. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6087 mL	13.0433 mL	26.0865 mL	65.2163 mL
	5 mM	0.5217 mL	2.6087 mL	5.2173 mL	13.0433 mL
	10 mM	0.2609 mL	1.3043 mL	2.6087 mL	6.5216 mL
	15 mM	0.1739 mL	0.8696 mL	1.7391 mL	4.3478 mL
	20 mM	0.1304 mL	0.6522 mL	1.3043 mL	3.2608 mL
	25 mM	0.1043 mL	0.5217 mL	1.0435 mL	2.6087 mL
	30 mM	0.0870 mL	0.4348 mL	0.8696 mL	2.1739 mL
	40 mM	0.0652 mL	0.3261 mL	0.6522 mL	1.6304 mL
	50 mM	0.0522 mL	0.2609 mL	0.5217 mL	1.3043 mL
	60 mM	0.0435 mL	0.2174 mL	0.4348 mL	1.0869 mL
	80 mM	0.0326 mL	0.1630 mL	0.3261 mL	0.8152 mL
	100 mM	0.0261 mL	0.1304 mL	0.2609 mL	0.6522 mL

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PT-2385

Publications Citing Use of MedChemExpress (MCE) PT-2385

All HIF/HIF Prolyl-Hydroxylase Isoforms