1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. PT2399

PT2399 

Cat. No.: HY-108697
Handling Instructions

PT2399 is an inhibitor of HIF2α.

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

PT2399 Chemical Structure

PT2399 Chemical Structure

CAS No. : 1672662-14-4

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Description

PT2399 is an inhibitor of HIF2α[1].

IC50 & Target

HIF2α[1]

In Vitro

PT2399 inhibits HIF2α directly causes tumor regression[1].
PT2399 binds directly to the HIF2α PAS B domain, and cripples HIF2α’s ability to bind to Aryl hydrocarbon receptor nuclear translocator (ARNT)[1].

Cell Viability Assay[1]

Cell Line: 786-O cells
Concentration: 0 μM, 0.2 μM, 20 μM
Incubation Time: 0-15 days
Result: Caused off-target toxicity because it inhibited the proliferation of HIF2α-/-786-O cells at 20 μM, and inhibited 786-O cell soft agar growth at 0.2 μM-2 μM.
In Vivo

PT2399 (100 mg/kg; oral gavage; every 12 hours) is more active than Sunitinib and inhibits tumor growth in several Sunitinib-resistant tumors in renal cell carcinoma (RCC) bearing mice[2].
PT2399 inhibits tumor cell proliferation 3.5 fold in RCC bearing mice[2].
PT2399 reduces tumor cell density and increases fibrosis in RCC bearing mice[2].

Animal Model: Mice with RCC tumorgraft[2]
Dosage: 100 mg/kg
Administration: Oral gavage; every 12 hours
Result: More active than sunitinib, and inhibited tumor growth in several sunitinib-resistant tumors.
Storage

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 200 mg/mL (476.96 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3848 mL 11.9241 mL 23.8481 mL
5 mM 0.4770 mL 2.3848 mL 4.7696 mL
10 mM 0.2385 mL 1.1924 mL 2.3848 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (3.98 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Molecular Weight

419.32

Formula

C₁₇H₁₀F₅NO₄S

CAS No.

1672662-14-4

SMILES

N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C(F)F)=O)C3=C2CC(F)(F)[[email protected]]3O)=C1

Shipping

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
PT2399
Cat. No.:
HY-108697
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PT2399

Cat. No.: HY-108697