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: 99.52%
COA 取扱説明書

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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Ipatasertib 構造式

Ipatasertib 構造式

CAS 番号 : 1001264-89-6

容量 価格(税別) 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 71 在庫あり
Solution
10 mM * 1 mL in DMSO USD 71 在庫あり
Solid
2 mg USD 50 在庫あり
5 mg USD 70 在庫あり
10 mg USD 100 在庫あり
50 mg USD 290 在庫あり
100 mg USD 450 在庫あり
200 mg USD 750 在庫あり
500 mg USD 1500 在庫あり
1 g USD 2600 在庫あり
5 g   お問い合わせ  
10 g   お問い合わせ  

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カスタマーレビュー

Based on 38 publication(s) in Google Scholar

Other Forms of Ipatasertib:

Top Publications Citing Use of Products

顧客検証

WB

    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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    • 生物活性

    • 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

    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)

    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.
    臨床実験
    分子量

    458.00

    分子式

    C24H32ClN5O2

    CAS 番号
    Appearance

    Solid

    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 : 220 mg/mL (480.35 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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    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: ≥ 2.08 mg/mL (4.54 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.54 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:  0.5% Methyl cellulose/0.5% Tween-80 in Saline water

      Solubility: 10 mg/mL (21.83 mM); Suspended solution; Need ultrasonic

    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: 99.88%

    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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    Ipatasertib Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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

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    製品名:
    Ipatasertib
    製品番号:
    HY-15186
    数量:
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