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

Ipatasertib tosylate  (Synonyms: GDC-0068 tosylate; RG7440 tosylate)

目录号: HY-15186C
产品使用指南

摩尔计算器

Ipatasertib (GDC-0068) tosylate 是一种口服有效的、高选择性和 ATP 竞争性泛 Akt 抑制剂，其对 Akt1/2/3 的 IC50 值分别为 5、18、8 nM。Ipatasertib 通过抑制 Akt 导致非 p53 依赖性的 PUMA 激活，从而同步激活 FoxO3a 和 NF-κB 。Ipatasertib 还能诱导癌细胞凋亡 (apoptosis)，抑制异种移植小鼠模型中的肿瘤生长。

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Ipatasertib tosylate Chemical Structure

Ipatasertib tosylate Chemical Structure

CAS No. : 1491138-24-9

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Ipatasertib tosylate 的其他形式现货产品:

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Ipatasertib tosylate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 39 篇科研文献

WB

    Ipatasertib tosylate purchased from MCE. 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 tosylate purchased from MCE. 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 tosylate purchased from MCE. 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.

    查看 Akt 亚型特异性产品:

    查看所有亚型
    Akt Akt1 Akt2 Akt3

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Ipatasertib (GDC-0068) tosylate 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 tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models[1][2].

    IC50 & Target

    Akt1

    5 nM (IC50)

    Akt2

    18 nM (IC50)

    Akt3

    8 nM (IC50)

    PKA

    3100 nM (IC50)

    体外研究
    (In Vitro)

    Ipatasertib tosylate (10 µM; 12, 24 h) 在细胞实验中，通过非 p53 依赖性的 PUMA 激活抑制结肠癌细胞增殖[1]。
    Ipatasertib tosylate (1, 5, 10, 20 μM; 24 h/10 μM; 3, 6, 12, 24 h) 在 HCT116 细胞中，以时间和浓度依赖的方式上调 PUMA 的表达[1]。
    Ipatasertib tosylate 在野生型、p53−/− 型, 以及 DLD1 (p53 突变) 型 HCT116 细胞中增加 PUMA 的 mRNA 水平[1]。
    Ipatasertib tosylate (10 µM; 24 h) 通过 PUMA/Bax 途径诱导 HCT116 细胞凋亡[1]。
    Cell Viability Assay:[1]

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

    Ipatasertib tosylate 相关抗体:

    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 WT, p53−/−, and DLD1 (p53 mutant) 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.
    体内研究
    (In Vivo)

    Ipatasertib tosylate (30 mg/kg; p.o.; single daily for 15 consecutive days) 在野生型和 PUMA−/− 型 HCT116 异种移植小鼠模型中显示出 PUMA 依赖性抗肿瘤活性[1]。

    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

    630.20

    Formula

    C31H40ClN5O5S
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Ipatasertib tosylate 相关分类

    • 摩尔计算器

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    • 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:

    Ipatasertib1491138-24-9GDC-0068RG7440GDC0068GDC 0068RG 7440RG-7440OrganoidAktApoptosisPKBProtein kinase BFoxO3aNF-κBPUMAp53HCT116 cellsapoptosisInhibitorinhibitorinhibit

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