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

Ipatasertib  (Synonyms: GDC-0068; RG7440)

目錄號(hào): HY-15186 純度: 99.79%
COA 產(chǎn)品使用指南 技術(shù)支持

Ipatasertib (GDC-0068) 是一種口服有效的、高選擇性和 ATP 競(jìng)爭(zhēng)性泛 Akt 抑制劑，其對(duì) Akt1/2/3 的 IC50 值分別為 5、18、8 nM。Ipatasertib 通過(guò)抑制 Akt 導(dǎo)致非 p53 依賴性的 PUMA 激活，從而同步激活 FoxO3a 和 NF-κB 。Ipatasertib 還能誘導(dǎo)癌細(xì)胞凋亡 (apoptosis)，抑制異種移植小鼠模型中的腫瘤生長(zhǎng)。

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Ipatasertib Chemical Structure

Ipatasertib Chemical Structure

CAS No. : 1001264-89-6

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     可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1209
In-stock
1 mg ￥449
In-stock
2 mg ￥650
In-stock
5 mg ￥1200
In-stock
10 mg ￥1800
In-stock
25 mg ￥3188
In-stock
50 mg ￥4800
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

Other Forms of Ipatasertib:

MCE 顧客使用本產(chǎn)品發(fā)表的 41 篇科研文獻(xiàn)

WB

    Ipatasertib 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 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 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 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    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)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    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]
    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 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 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]
    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]
    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 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 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]
    體外研究
    (In Vitro)

    Ipatasertib (10 μM; 12, 24 h) 在細(xì)胞實(shí)驗(yàn)中，通過(guò)非 p53 依賴性的 PUMA 激活抑制結(jié)腸癌細(xì)胞增殖[1]。
    Ipatasertib (1, 5, 10, 20 μM; 24 h/10 μM; 3, 6, 12, 24 h) 在 HCT116 細(xì)胞中，以時(shí)間和濃度依賴的方式上調(diào) PUMA 的表達(dá)[1]。
    Ipatasertib 在野生型、p53?/? 型, 以及 DLD1 (p53 突變) 型 HCT116 細(xì)胞中增加 PUMA 的 mRNA 水平[1]。
    Ipatasertib (10 μM; 24 h) 通過(guò) PUMA/Bax 途徑誘導(dǎo) HCT116 細(xì)胞凋亡[1]。

    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.
    體內(nèi)研究
    (In Vivo)

    Ipatasertib (30 mg/kg; p.o.; single daily for 15 consecutive days) 在野生型和 PUMA?/? 型 HCT116 異種移植小鼠模型中顯示出 PUMA 依賴性抗腫瘤活性[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.
    Clinical Trial
    分子量

    458.00

    Formula

    C24H32ClN5O2
    CAS 號(hào)
    性狀

    固體

    顏色

    White to light yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 100 mg/mL (218.34 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

    H2O 中的溶解度 : 3.57 mg/mL (7.79 mM; 超聲助溶 (<60°C))

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 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
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (10.92 mM); 澄清溶液

      此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (10.92 mM); 澄清溶液

      此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 0.5% Methyl cellulose/0.5% Tween-80 in Saline water

      Solubility: 10 mg/mL (21.83 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.88%

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 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

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    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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