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PT2399 HIF antagonist

Cat.No.S8351

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

Chemical Structure

Molecular Weight: 419.32

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (200.32 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 419.32 Formula

C17H10F5NO4S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1672662-14-4 -- Storage of Stock Solutions

Synonyms N/A Smiles C1C2=C(C=CC(=C2C(C1(F)F)O)S(=O)(=O)C(F)F)OC3=CC(=CC(=C3)C#N)F

Mechanism of Action

Targets/IC50/Ki
HIF-2α
HIF-1β
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

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 this compound in resistant tumors. Sensitive tumors exhibits a distinguishing gene expression signature, and generally higher HIF-2α levels. Prolonged treatment with this chemical leads to resistance.
References

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