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

PT2399 

Cat. No.: HY-108697 Purity: 99.88% ee.: 96.37%
Handling Instructions

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.

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

PT2399 Chemical Structure

PT2399 Chemical Structure

CAS No. : 1672662-14-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3350 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2][3].

IC50 & Target

IC50: 6 nM (HIF-2α)[3]

In Vitro

PT2399 (compound 10f) inhibits HIF-2α with an IC50 of 6 nM[3].
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].
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].
PT2399 (0.2–2 μM; 0-21 days) inhibits 786-O cells soft agar growth[2].
PT2399 represses various HIF target genes in 786-O VHL−/− ccRCC cells, does not suppress HIF-1α-specific targets such as BNIP3[2].

Cell Viability Assay[1]

Cell Line: 786-O cells
Concentration: 0 μM, 0.2 μM, 2 μM
Incubation Time: 0-21 days
Result: Inhibited 786-O cell soft agar growth at 0.2–2 μM.
In Vivo

PT2399 inhibits tumor cell proliferation 3.5 fold in renal cell carcinoma (RCC) bearing mice[1].
PT2399 reduces tumor cell density and increases fibrosis in RCC bearing mice[1].
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].

Animal Model: Mice with RCC tumorgraft[1]
Dosage: 100 mg/kg
Administration: Oral gavage; every 12 hours
Result: More active than SU 11248, and inhibited tumor growth in several SU 11248-resistant tumors.
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

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    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

  • 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

Purity: 99.88% ee.: 96.37%

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PT2399
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HY-108697
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