Home Angiogenesis HIF antagonist PT2399 For research use only.

PT2399

PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β.

PT2399 Chemical Structure

PT2399 Chemical Structure

CAS No. 1672662-14-4

Purity & Quality Control

Batch: S835101 DMSO]84 mg/mL]false]Ethanol]84 mg/mL]false]Water]Insoluble]false Purity: 99.93%
99.93

PT2399 Related Products

Signaling Pathway

HIF Signaling Pathways

HIF Signaling Pathway

Biological Activity

Description PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β.
Targets
HIF-2α [1] HIF-1β [1]
In vitro
In vitro

PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β.
In Vivo
In vivo

PT2399 dissociates HIF-2 (an obligatory heterodimer [HIF-2α/HIF-1β])14 in human Clear cell Renal Cell Carcinoma (ccRCC) suppressing tumorigenesis in 56% (10/18) lines. Illustrating drug specificity, gene expression is largely unaffected by PT2399 in resistant tumors. Sensitive tumors exhibits a distinguishing gene expression signature, and generally higher HIF-2α levels. Prolonged PT2399 treatment leads to resistance.[2]
Animal Research Animal Models 4–6 week old female/male NOD/SCID mice
Dosages 100 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 419.32 Formula

C17H10F5NO4S
CAS No. 1672662-14-4 SDF --
Smiles C1C2=C(C=CC(=C2C(C1(F)F)O)S(=O)(=O)C(F)F)OC3=CC(=CC(=C3)C#N)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 84 mg/mL ( (200.32 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 84 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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