2. PI3K/Akt/mTOR
  3. PI3K mTOR
  4. Paxalisib

Paxalisib  (Synonyms: GDC-0084)

製品番号: HY-19962 純度: 99.51%
COA 取扱説明書 Technical Support

Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1382979-44-3

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 77 在庫あり
Solution
10 mM * 1 mL in DMSO USD 77 在庫あり
Solid
5 mg $70 在庫あり
10 mg $110 在庫あり
25 mg $230 在庫あり
50 mg $370 在庫あり
100 mg $680 在庫あり
200 mg   お問い合わせ  
500 mg   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

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Paxalisib 関連抗体

Top Publications Citing Use of Products

    Paxalisib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Nov 30:1-21.  [Abstract]

    Paxalisib (72 h) reduced the viability of both U251 and U87 cells with IC50 values of 1.551 μM and 1.371 μM, respectively.

    Paxalisib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Nov 30:1-21.  [Abstract]

    Paxalisib (1–2 μM; 24 h) reduced the expression levels of IDH1 and CCND1 in U251 and U87 cells.

    Paxalisib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Nov 30:1-21.  [Abstract]

    Representative bright-field microscopy images of patient-derived GSC#40 treated with DMSO (control), Paxalisib (2 μM), or metformin (10 mM) at days 1, 3, and 7 of culture. Scale bar: 400 mm. The results showed that Paxalisib (2 μM) significantly retarded the growth of cell spheroids throughout the seven-day observation period.

    Paxalisib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Nov 30:1-21.  [Abstract]

    Immunofluorescence analysis showing colocalization of IDH1 (red) and LAMP1 (green) in GSC#40 treated with DMSO (control), Paxalisib (2 μM), or metformin (10 mM) for 7 days. White arrows indicate co-localized puncta, indicating lysosomal trafficking of IDH1. DAPI (blue) was used for nuclei staining. Original magnification: 100x. Scale bar: 40 μm.

    Paxalisib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1941-1948.  [Abstract]

    Paxalisib (GDC-0084, 100-1000 nM; 30 h) significantly upregulated the expression of cleaved-caspase-3 and cleaved-caspase-9 in treated A431 cells.

    Paxalisib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1941-1948.  [Abstract]

    Paxalisib (GDC-0084, 100–1000 nM; 72 h) inhibited the survival of all cSCC cells.

    Paxalisib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1941-1948.  [Abstract]

    Paxalisib (GDC-0084, 10-1000 nM; 30 h) treatment in A431 cells dose-dependently increased the activities of caspase-3 and caspase-9.

    Paxalisib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1941-1948.  [Abstract]

    Paxalisib (GDC-0084, 10-1000 nM; 48 h) dose-dependently increased histone-bound DNA ELISA OD in A431 cells.

    Paxalisib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1941-1948.  [Abstract]

    Paxalisib (GDC-0084, 500 nM; 48 h) induced apoptosis activation in A431 cells.

    PI3K 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
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    mTOR 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
    mTOR mTORC1 mTORC2

    • 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

    Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively[1].

    IC50 & Target[1]

    PI3Kα

    2 nM (Ki)

    PI3Kδ

    3 nM (Ki)

    PI3Kγ

    10 nM (Ki)

    PI3Kβ

    46 nM (Ki)

    mTOR

    70 nM (Ki)

    Cellular Effect
    Cell Line Type Value Description References
    PC-3 EC50
    0.4 μM
    Compound: 16
    Antiproliferative activity against human PC3 cells after 3 days by CellTitre-Glo assay
    Antiproliferative activity against human PC3 cells after 3 days by CellTitre-Glo assay
    		[PMID: 27096040]
    SF-268 EC50
    1.01 μM
    Compound: 16
    Antiproliferative activity against human SF268 cells after 4 days by CellTitre-Glo assay
    Antiproliferative activity against human SF268 cells after 4 days by CellTitre-Glo assay
    		[PMID: 27096040]
    U-87MG ATCC EC50
    0.74 μM
    Compound: 16
    Antiproliferative activity against human U87 cells after 4 days by CellTitre-Glo assay
    Antiproliferative activity against human U87 cells after 4 days by CellTitre-Glo assay
    		[PMID: 27096040]
    体外実験

    Paxalisib (GDC-0084; Compound 16) maintains inhibition of each of the Class I PI3K isoforms but with more potent inhibition of mTOR. Paxalisib is also tested in five different GBM cell lines and is found to have antiproliferative EC50s ranging from 0.3 to 1.1 μM[1].

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

    Paxalisib 関連抗体
    体内実験

    After a 25 mg/kg dose of Paxalisib (GDC-0084; Compound 16) administered orally, pAKT in normal mouse brain tissue is significantly inhibited at 1 and 6 h postdose. The potent inhibition of pAKT at both time points in this study demonstrates that Paxalisib inhibits its target behind a fully intact BBB. In addition to the pharmacodynamic effect in normal brain tissue, Paxalisib is studied in a subcutaneous U87 tumor xenograft model of glioblastoma in mice. In this study, Paxalisib achieves significant and dose-dependent tumor growth inhibition. Tumor growth inhibition is first observed at a 2.2 mg/kg dose level. Higher doses led to greater tumor growth inhibition, including tumor regressions at the 17.9 mg/kg dose level. Each of these doses is well tolerated for the duration of the study[1].

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

    382.42

    分子式

    C18H22N8O2
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC1=NC=C(C2=NC(N3CCOCC3)=C4N=C(C(C)(C)OCC5)N5C4=N2)C=N1
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 7.69 mg/mL (20.11 mM; ultrasonic and warming and heat to 60°C; 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 2.6149 mL 13.0746 mL 26.1493 mL
    5 mM 0.5230 mL 2.6149 mL 5.2299 mL
    10 mM 0.2615 mL 1.3075 mL 2.6149 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. 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

    ×
    体積 （終了）

    V2

    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 mg/mL (2.61 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: 1 mg/mL (2.61 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (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).
    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: 99.51%

    COA (258 KB) HNMR (258 KB) LCMS (266 KB)

    取扱説明書 (2659 KB)
    参考文献
    動物実験
    [1]

    Mice[1]
    PTEN-null U-87 MG/M human glioblastoma cancer cells are cultured in RPMI 1640 media plus 1% L-glutamine with 10% fetal bovine serum. Cells in log-phase growth are harvested and resuspended in HBSS:Matrigel (1:1, v:v) for injection into female NCr nude mice aged 20 weeks. Animals receive five million cells subcutaneously in the right lateral thorax in 0.1 mL. Mice bearing established tumors in the range of 200-500 mm3 are separated into groups of equally sized tumors (n=6-7/group) to receive escalating doses of Paxalisib. Paxalisib is formulated once weekly in 0.5% methylcellulose and 0.2% Tween-80 at concentrations needed for target doses in a volume of 0.2 mL. All formulations are stored in a refrigerator and brought to room temperature and mixed well by vortex before oral administration by gavage once daily for 23 days. Tumor volumes are calculated. Changes in body weights are reported as a percentage change from the starting weight.

    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. 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 2.6149 mL 13.0746 mL 26.1493 mL 65.3731 mL
    5 mM 0.5230 mL 2.6149 mL 5.2299 mL 13.0746 mL
    10 mM 0.2615 mL 1.3075 mL 2.6149 mL 6.5373 mL
    15 mM 0.1743 mL 0.8716 mL 1.7433 mL 4.3582 mL
    20 mM 0.1307 mL 0.6537 mL 1.3075 mL 3.2687 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Paxalisib 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:

    Paxalisib1382979-44-3GDC-0084GDC0084GDC 0084PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

    		  

    カスタマ需要量 *

    お名前 *

    		 

    タイトル

    メールアドレス *

    		 

    電話番号 *

    デパートメント

    		 

    組纖名 *

    市区町村

    都道府県

    国或いは地域 *

    		      

    必ず会社名を記載ください。個人への返信は行いません。

    備考

    バルクお問い合わせ

    Inquiry Information

    製品名:
    Paxalisib
    製品番号:
    HY-19962
    数量:
    MCE 日本正規代理店:

    カスタマーレビュー

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    製品名

    		  

    Lot #

    お名前 *

    		 

    メールアドレス *

    電話番号 *

    		 

    部門 *

    組纖名 *

    		 

    国或いは地域 *

    備考

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.