1. Stem Cell/Wnt PI3K/Akt/mTOR Apoptosis
  2. Organoid Akt Apoptosis
  3. Ipatasertib

Ipatasertib  (Synonyms: GDC-0068; RG7440)

製品番号: HY-15186 純度: 99.74%
COA 取扱説明書 Technical Support

Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models.

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CAS 番号 : 1001264-89-6

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>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 85 在庫あり
Solution
10 mM * 1 mL in DMSO USD 85 在庫あり
Solid
2 mg $60 在庫あり
5 mg $84 在庫あり
10 mg $120 在庫あり
25 mg $245 在庫あり
50 mg $348 在庫あり
100 mg $540 在庫あり
200 mg $900 在庫あり
500 mg $1800 在庫あり
1 g $3120 在庫あり
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カスタマーレビュー

Based on 60 publication(s) in Google Scholar

Other Forms of Ipatasertib:

Top Publications Citing Use of Products

顧客検証

WB
Cell Proliferation/Viability Assay

    Ipatasertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 25;16(1):1774.  [Abstract]

    Viable cell numbers and PUFA-PC ratio after treatment with LY294002 (iPI3K, 10 µM), picropodophyllin (iRTK, 10 µM), ipatasertib (iAkt, 10 µM), or fatostatin (iSREBP1, 20 µM) for 48 h.

    Ipatasertib purchased from MedChemExpress. Usage Cited in: Front Oncol. 2021 Nov 24:11:766298.  [Abstract]

    Ipatasertib (0.625, 1.25, 5 µM; 24 h) increases the phosphorylation of AKT in MFM-223 FGFR2amp cells.

    Ipatasertib purchased from MedChemExpress. Usage Cited in: Skelet Muscle. 2021 Mar 15;11(1):6.  [Abstract]

    The western blot analysis and quantification of phosphorylated and all forms of AKT and P70, MyoG, and MyoD, after transfecting miR-1290/miR-NC with or without GDC0068. GDC-0068 inhibits miR-1290-activated phosphorylation of AKT and P70 in C2C12 myoblasts.

    Ipatasertib purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2020 Oct;180:114145.  [Abstract]

    C2C12 myoblasts were pre-incubated with 2.5 μM GDC-0068 for 30 min then treated with 0.2 μM S-Rg3. After incubation with S-Rg3 for 72 h and 24 h, Western blotting is used to detect levels of Myf5 and myogenin in C2C12 myoblasts after incubation of cells with S-Rg3 for 120 h. GDC-0068 inhibits S-Rg3-activated phosphorylation of Akt and mTOR in C2C12 myoblasts.

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    • 参考文献

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    製品説明

    Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models[1][2].

    IC50 & Target[2]

    Akt1

    5 nM (IC50)

    Akt3

    8 nM (IC50)

    Akt2

    18 nM (IC50)

    PKA

    3100 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    AN3-CA EC50
    925 nM
    Compound: Ipatasertib
    Antiproliferative activity against human AN3-CA cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    Antiproliferative activity against human AN3-CA cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    [PMID: 30996949]
    BT-474 EC50
    2371 nM
    Compound: Ipatasertib
    Antiproliferative activity against human BT-474 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    Antiproliferative activity against human BT-474 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    [PMID: 30996949]
    BT-474 GI50
    0.3 μM
    Compound: GDC-0068
    Antiproliferative activity against human BT-474 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
    Antiproliferative activity against human BT-474 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
    [PMID: 34855399]
    C-33-A IC50
    725.97 nM
    Compound: GDC-0068
    Antiproliferative activity against human C-33-A habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    Antiproliferative activity against human C-33-A habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    [PMID: 35679512]
    CAL-51 IC50
    265.2 nM
    Compound: GDC-0068
    Antiproliferative activity against human CAL-51 habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    Antiproliferative activity against human CAL-51 habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    [PMID: 35679512]
    Hep 3B2 IC50
    389 μM
    Compound: GDC-0068
    Cytotoxicity against human Hep3B cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against human Hep3B cells assessed as reduction in cell viability by MTT assay
    [PMID: 32007668]
    HepG2 IC50
    0.268 μM
    Compound: GDC-0068
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
    [PMID: 32007668]
    Huh-7 IC50
    0.167 μM
    Compound: GDC-0068
    Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by MTT assay
    [PMID: 32007668]
    KU-19-19 EC50
    24037 nM
    Compound: Ipatasertib
    Antiproliferative activity against human KU-19-19 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    Antiproliferative activity against human KU-19-19 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    [PMID: 30996949]
    LNCaP IC50
    157 nM
    Compound: 28, GDC-0068
    Inhibition of Akt1 in human LNCAP cells assessed as phosphorylation of PRAS40 at Thr246 after 1.5 hrs
    Inhibition of Akt1 in human LNCAP cells assessed as phosphorylation of PRAS40 at Thr246 after 1.5 hrs
    [PMID: 22934575]
    LNCaP IC50
    95 nM
    Compound: 28, GDC-0068
    Cytotoxicity against human LNCAP cells assessed as reduction of resazurin to resorufin after 72 hrs
    Cytotoxicity against human LNCAP cells assessed as reduction of resazurin to resorufin after 72 hrs
    [PMID: 22934575]
    MCF7 EC50
    5036 nM
    Compound: Ipatasertib
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    [PMID: 30996949]
    MCF7 IC50
    1 μM
    Compound: 28, GDC-0068
    Cytotoxicity against human MCF7 cells overexpressing Her2 assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay
    Cytotoxicity against human MCF7 cells overexpressing Her2 assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay
    [PMID: 22934575]
    MDA-MB-468 GI50
    3.7 μM
    Compound: GDC-0068
    Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
    Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
    [PMID: 34855399]
    NCI-H1975 IC50
    >20 μM
    Compound: 2; GDC-0068
    Antiproliferative activity against human osimertinib resistant NCI-H1975 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay
    Antiproliferative activity against human osimertinib resistant NCI-H1975 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay
    [PMID: 36173763]
    PC-3 GI50
    7.6 μM
    Compound: GDC-0068
    Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
    Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
    [PMID: 34855399]
    PC-3 IC50
    1 μM
    Compound: 28, GDC-0068
    Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay
    Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay
    [PMID: 22934575]
    PC-3 IC50
    3544.33 nM
    Compound: GDC-0068
    Antiproliferative activity against human PC-3 habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    Antiproliferative activity against human PC-3 habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    [PMID: 35679512]
    RL95-2 IC50
    331.07 nM
    Compound: GDC-0068
    Antiproliferative activity against human RL95-2 habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    Antiproliferative activity against human RL95-2 habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    [PMID: 35679512]
    SMMC-7721 IC50
    0.661 μM
    Compound: GDC-0068
    Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability by MTT assay
    [PMID: 32007668]
    T47D EC50
    443 nM
    Compound: Ipatasertib
    Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    [PMID: 30996949]
    T47D IC50
    327.77 nM
    Compound: GDC-0068
    Antiproliferative activity against human T47D habouring PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    Antiproliferative activity against human T47D habouring PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    [PMID: 35679512]
    TOV21G IC50
    715.2 nM
    Compound: GDC-0068
    Antiproliferative activity against human TOV-21G habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    Antiproliferative activity against human TOV-21G habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    [PMID: 35679512]
    ZR-75-1 EC50
    219 nM
    Compound: Ipatasertib
    Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
    [PMID: 30996949]
    ZR-75-1 IC50
    1316 nM
    Compound: GDC-0068
    Antiproliferative activity against human ZR-75-1 habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    Antiproliferative activity against human ZR-75-1 habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
    [PMID: 35679512]
    体外実験

    Ipatasertib (10 µM; 12, 24 h) suppresses colon cancer cell proliferation by p53 irrespectively activating PUMA in vitro[1].
    Ipatasertib (1, 5, 10, 20 μM; 24 h/10 μM; 3, 6, 12, 24 h) up-regulates the expression level of PUMA in a concentration and time dependent manner in HCT116 cells[1].
    Ipatasertib increases the mRNA level of PUMA in HCT116 WT, p53−/−, and DLD1 (p53 mutant) cells[1].
    Ipatasertib (10 µM; 24 h) induces apoptosis through PUMA/Bax pathway in HCT116 cells[1].

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

    Cell Viability Assay[1]

    Cell Line: HCT116 WT, p53−/−, and DLD1 (p53 mutant) cells
    Concentration: 10 µM
    Incubation Time: 12, 24 h
    Result: Decreased all the three cell lines viability.

    Apoptosis Analysis[1]

    Cell Line: HCT116 cells
    Concentration: 10 µM
    Incubation Time: 24 h
    Result: Induced apoptosis through PUMA/Bax pathway.

    Western Blot Analysis[1]

    Cell Line: HCT116 cells
    Concentration: 1, 5, 10, 20 μM for 24 h/10 μM for 3, 6, 12, 24 h
    Incubation Time: 24 h; 3, 6, 12, 24 h
    Result: Increased the level of PUMA in a concentration and time dependent manner.
    体内実験

    Ipatasertib (30 mg/kg; p.o.; single daily for 15 consecutive days) exhibits PUMA-dependent antitumor activity in HCT116 WT and PUMA−/− cells xenograft nude mice model[1].

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

    Animal Model: HCT116 WT and PUMA−/− cells xenograft nude mice model[1].
    Dosage: 30 mg/kg
    Administration: Oral gavage; single daily for 15 consecutive days.
    Result: Inhibited growth of tumors in a PUMA-dependent manner.
    分子量

    458.00

    分子式

    C24H32ClN5O2

    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    ClC1=CC=C([C@@H](CNC(C)C)C(N2CCN(C3=C([C@H](C)C[C@H]4O)C4=NC=N3)CC2)=O)C=C1

    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 : 100 mg/mL (218.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 3.57 mg/mL (7.79 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1834 mL 10.9170 mL 21.8341 mL
    5 mM 0.4367 mL 2.1834 mL 4.3668 mL
    10 mM 0.2183 mL 1.0917 mL 2.1834 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * 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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    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 (10.92 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 (10.92 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.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    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: 99.88%

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.1834 mL 10.9170 mL 21.8341 mL 54.5852 mL
    5 mM 0.4367 mL 2.1834 mL 4.3668 mL 10.9170 mL
    DMSO 10 mM 0.2183 mL 1.0917 mL 2.1834 mL 5.4585 mL
    15 mM 0.1456 mL 0.7278 mL 1.4556 mL 3.6390 mL
    20 mM 0.1092 mL 0.5459 mL 1.0917 mL 2.7293 mL
    25 mM 0.0873 mL 0.4367 mL 0.8734 mL 2.1834 mL
    30 mM 0.0728 mL 0.3639 mL 0.7278 mL 1.8195 mL
    40 mM 0.0546 mL 0.2729 mL 0.5459 mL 1.3646 mL
    50 mM 0.0437 mL 0.2183 mL 0.4367 mL 1.0917 mL
    60 mM 0.0364 mL 0.1820 mL 0.3639 mL 0.9098 mL
    80 mM 0.0273 mL 0.1365 mL 0.2729 mL 0.6823 mL
    100 mM 0.0218 mL 0.1092 mL 0.2183 mL 0.5459 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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    一般には略語で表示されます:C1V1 = C2V2

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    製品名:
    Ipatasertib
    製品番号:
    HY-15186
    数量:
    MCE 日本正規代理店: