2. Metabolic Enzyme/Protease Autophagy
  3. HIF/HIF Prolyl-Hydroxylase Autophagy
  4. PX-478

PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.

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CAS 番号 : 685898-44-6

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10 mg $168 在庫あり
25 mg $260 在庫あり
50 mg $350 在庫あり
100 mg $550 在庫あり
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カスタマーレビュー

Based on 95 publication(s) in Google Scholar

Other Forms of PX-478:

PX-478 関連抗体

Top Publications Citing Use of Products

顧客検証

WB
IHC
Cell Migration/Invasion Assay
IF

    PX-478 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2025 May 12;43(5):937-954.e9.  [Abstract]

    IHC of MT2A in HCT116-bearing mice treated with ES + Cu (0.25 mg/kg, per day, i.p.) and PX-478 (20 mg/kg per day, i.p.).

    PX-478 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681.  [Abstract]

    Control and ASH1L-F3-overexpressing LNCaP cells were treated with Vehicle (Veh) or HIF-1α inhibitors LW6 (15 μM), 2-MeOE2 (2-ME, 25 μM), or PX-478 (20 μM) for 48 h in the presence of CoCl2 (200uM), followed by migration assays. n = 3 biological replicates per group. Scale bar = 1000 μm.

    PX-478 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681.  [Abstract]

    PX-478 (40 mg/kg; i.p.; thrice weekly for three weeks) abrogates the significant inhibition of intraosseous tumor growth induced by ASH1L knockdown in C57BL/6J mice.

    PX-478 purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2020 Apr 8;12(538):eaay1620.  [Abstract]

    Representative pimonidazole staining of kidney sections from 16-week-old MRL/lpr mice treated with PBS or PX-478, and quantification of pimonidazole-positive cortical tubular cells.

    PX-478 purchased from MedChemExpress. Usage Cited in: Front Immunol. 2018 Jul 23:9:1667.  [Abstract]

    Manipulation of the protein level of hypoxia-inducible factor 1 alpha (HIF-1α) in NR8383. 50 µM PX478 treatment for 20 h is used to downregulate the HIF-1α protein level in NR8383 cells (A). 1 mM DMOG treatment for 8 h is used to upregulate the HIF-1α protein level in NR8383 cells (B).

    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

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier[1][2].

    IC50 & Target

    HIF-1α[1]
    Cellular Effect
    Cell Line Type Value Description References
    MCF7 IC50
    19.7 μM
    Compound: PX-478
    Antiproliferative activity against human MCF7 cells after 72 hrs under hypoxic condition by MTT assay
    Antiproliferative activity against human MCF7 cells after 72 hrs under hypoxic condition by MTT assay
    		[PMID: 28209257]
    MDA-MB-231 IC50
    62.8 μM
    Compound: PX-478
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs under hypoxic condition by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs under hypoxic condition by MTT assay
    		[PMID: 28209257]
    MDA-MB-468 IC50
    45.1 μM
    Compound: PX-478
    Antiproliferative activity against human MDA-MB-468 cells after 72 hrs under hypoxic condition by MTT assay
    Antiproliferative activity against human MDA-MB-468 cells after 72 hrs under hypoxic condition by MTT assay
    		[PMID: 28209257]
    体外実験

    PC3 and DU 145 cells express HIF-1α protein are treated with PX-478 for 20 hr under normoxia. PC3 cells are more sensitive to PX-478 as compared with DU 145 cells. Densitometric analysis shows that the IC50 for HIF-1α inhibition for PC3 cells under normoxic condition is 20-25 μM, whereas the IC50 for HIF-1α inhibition for the DU 145 cells is 40-50 μM. PC3 and DU 145 cells are treated with different concentrations of PX-478 (10, 20, 30, 40, 50, and 60 μM) for 18-20 hr under normoxia or hypoxia. Under normoxia, PC3 cells are more sensitive to PX-478 than DU 145 cells. IC50 for clonogenic survival (n=3) is 17 μM for PC3 cells and 35 μM for DU 145 cells. When cells are treated with the drug under hypoxic condition for 18 hr, the IC50 is 16 μM for PC3 cells and 22 μM for DU 145 cells. Thus DU 145 cells are more sensitive to PX-478 under hypoxic condition[1].

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

    PX-478 関連抗体
    体内実験

    PX-478 is administered to mice with congenital heart disease (Nfatc1-Cre/caACVR1fl/fl) every other day starting from birth for 2 wk. Treated mice have significantly less ectopic bone at the ankle joints compared with mutant mice treated with vehicle (6.8 mm3 vs. 2.2 mm3, P<0.01)[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    394.12

    分子式

    C13H20Cl4N2O3
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    [O-][N+](CCCl)(CCCl)C(C=C1)=CC=C1C[C@H](N)C(O)=O.Cl.Cl
    輸送条件

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

    -20°C, stored under nitrogen, away from moisture

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

    H2O : 100 mg/mL (253.73 mM; Need ultrasonic)

    DMSO : 100 mg/mL (253.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5373 mL 12.6865 mL 25.3730 mL
    5 mM 0.5075 mL 2.5373 mL 5.0746 mL
    10 mM 0.2537 mL 1.2686 mL 2.5373 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, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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    Volume
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    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）

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    体積 （開始）

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    濃度 （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: ≥ 5 mg/mL (12.69 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (12.69 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  Saline

      Solubility: 16.67 mg/mL (42.30 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

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    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    純度とドキュメンテーション

    純度: 99.58%

    COA (251 KB) HNMR (376 KB) RP-HPLC (278 KB) MS (72 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [1]

    To determine the effect of PX-478 in combination with radiation, cells are treated with PX-478 for 24 hr under normoxic condition, irradiated and plated after 1 hr. Colonies are stained with crystal violet after 12 days and the colonies of >50 cells are counted. For combination treatments, net survival is calculated by correcting the toxicity of PX-478 alone. Enhancement factor (EF) is calculated by dividing the dose of radiation required to reduce plating efficiency to 10% when cells are treated with radiation alone by the dose of radiation required to reduce plating efficiency to 10% when cells are treated with PX-478 and radiation[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [2]

    Mice[2]
    Burn/tenotomy or hybrid HO mice are administered PX-478 (100 mg/kg) or Rapamycin (5 mg/kg) in PBS solution via intraperitoneal injection. Mice receive injections every other day for the duration of the study. Nfatc1-Cre/caACVR1fl/wt mice are administered PX-478 (100 mg/kg) every other day for a total of 2 wk.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    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, away from moisture). 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
    H2O / DMSO 1 mM 2.5373 mL 12.6865 mL 25.3730 mL 63.4325 mL
    5 mM 0.5075 mL 2.5373 mL 5.0746 mL 12.6865 mL
    10 mM 0.2537 mL 1.2686 mL 2.5373 mL 6.3432 mL
    15 mM 0.1692 mL 0.8458 mL 1.6915 mL 4.2288 mL
    20 mM 0.1269 mL 0.6343 mL 1.2686 mL 3.1716 mL
    25 mM 0.1015 mL 0.5075 mL 1.0149 mL 2.5373 mL
    30 mM 0.0846 mL 0.4229 mL 0.8458 mL 2.1144 mL
    40 mM 0.0634 mL 0.3172 mL 0.6343 mL 1.5858 mL
    50 mM 0.0507 mL 0.2537 mL 0.5075 mL 1.2686 mL
    60 mM 0.0423 mL 0.2114 mL 0.4229 mL 1.0572 mL
    80 mM 0.0317 mL 0.1586 mL 0.3172 mL 0.7929 mL
    100 mM 0.0254 mL 0.1269 mL 0.2537 mL 0.6343 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    PX-478 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    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）
    × = ×
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    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:

    PX-478685898-44-6PX478PX 478HIF/HIF Prolyl-HydroxylaseAutophagyHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
    HY-10231
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