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

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.

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PT2399

PT2399 構造式

CAS 番号 : 1672662-14-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 在庫あり
Solution
10 mM * 1 mL in DMSO USD 330 在庫あり
Solid
5 mg $300 在庫あり
10 mg $450 在庫あり
25 mg $765 在庫あり
50 mg $1200 在庫あり
100 mg $1680 在庫あり
200 mg $2185 在庫あり
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 11 publication(s) in Google Scholar

Other Forms of PT2399:

PT2399 関連抗体

Top Publications Citing Use of Products

HIF/HIF Prolyl-Hydroxylase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
HIF-1α HIF PHD1

  • 生物活性

  • 純度とドキュメンテーション

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製品説明

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]
体外実験

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].

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

PT2399 関連抗体

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.
体内実験

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].

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

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.
分子量

419.32

分子式

C17H10F5NO4S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, stored under nitrogen

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

DMSO : ≥ 200 mg/mL (476.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

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体積 （終了）

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体内:

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

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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.96% ee.: 100.00%

COA (253 KB) HNMR (190 KB) NP-HPLC (291 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3848 mL 11.9241 mL 23.8481 mL 59.6203 mL
5 mM 0.4770 mL 2.3848 mL 4.7696 mL 11.9241 mL
10 mM 0.2385 mL 1.1924 mL 2.3848 mL 5.9620 mL
15 mM 0.1590 mL 0.7949 mL 1.5899 mL 3.9747 mL
20 mM 0.1192 mL 0.5962 mL 1.1924 mL 2.9810 mL
25 mM 0.0954 mL 0.4770 mL 0.9539 mL 2.3848 mL
30 mM 0.0795 mL 0.3975 mL 0.7949 mL 1.9873 mL
40 mM 0.0596 mL 0.2981 mL 0.5962 mL 1.4905 mL
50 mM 0.0477 mL 0.2385 mL 0.4770 mL 1.1924 mL
60 mM 0.0397 mL 0.1987 mL 0.3975 mL 0.9937 mL
80 mM 0.0298 mL 0.1491 mL 0.2981 mL 0.7453 mL
100 mM 0.0238 mL 0.1192 mL 0.2385 mL 0.5962 mL
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PT2399 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PT23991672662-14-4PT 2399PT-2399HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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製品番号:
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