Ipatasertib (GDC-0068)

目录号:S2808 别名: RG7440

Ipatasertib (GDC-0068) Chemical Structure

Molecular Weight(MW): 458

Ipatasertib (GDC-0068)是一种高选择性的pan-Akt抑制剂,靶向作用于Akt1/2/3,在无细胞试验中IC50为5 nM/18 nM/8 nM,比作用于PKA选择性高620倍。Phase 2。

规格 价格 库存 购买数量  
RMB 3094.44 现货
RMB 2192.93 现货
RMB 3025.41 现货
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客户使用Selleck该产品发表文献8篇:

客户使用该产品的3个实验数据:

  • Inhibition of AKT signaling abolishes MKK4 phosphorylation on Ser78 in injured axons. Cultures of sensory neurons were treated with 5 µM MK-2206 or 5 µM GDC-0068 for 1 hr prior to axotomy. Axonal proteins harvested at indicated time points after axotomy were subjected to immunoblot analysis.

    Cell, 2015, 160(1-2): 161-76 . Ipatasertib (GDC-0068) purchased from Selleck.

    The functional significance of the PI3K/Akt pathway in CCR5-mediated DNA damage signaling was assessed using the ATP-competitive, small-molecule pan-Akt inhibitor (ipatasertib) and or the CCR5 inhibitor Maraviroc in doxorubicin-treated cells. Western blot analysis was conducted as shown for SUM-159 cells (B) and MDA-MB-175VII (doxorubicin-resistant breast cancer cells) (D).

    Clin Cancer Res, 2018, 78(7):1657-1671. Ipatasertib (GDC-0068) purchased from Selleck.

  • In vitro evaluation of BAR activity in A549-BAR cell line. (A) Bioluminescence activity was quantified 1 hour after treatment in response to various compounds at two concentrations (n = 6). (B) Western blotting analysis after 1 hour of treatment showing the expression of pAKT (Ser473), AKT, pPRAS40 (Thr246), RAS40, pGSK3β (Ser9), GSK3β, pEGFR (Tyr1068), EGFR, and β-Actin of whole cell lysates.

    Neoplasia, 2017, 19(4):310-320. Ipatasertib (GDC-0068) purchased from Selleck.

产品安全说明书

Akt抑制剂选择性比较

生物活性

产品描述 Ipatasertib (GDC-0068)是一种高选择性的pan-Akt抑制剂,靶向作用于Akt1/2/3,在无细胞试验中IC50为5 nM/18 nM/8 nM,比作用于PKA选择性高620倍。Phase 2。
靶点
Akt1 [1]
(Cell-free assay)
Akt3 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
5 nM 8 nM 18 nM
体外研究

对一大组230种激酶测试,GDC-0068只抑制3种激酶,浓度为 1 μM 时抑制70%以上,(抑制PRKG1α,PRKG1β,和p70S6K时, IC50分别为98 nM, 69 nM, 和 860 nM)。GDC-0068 作用于Akt比作用于PKA 选择性高100倍以上,抑制Akt时 IC50为3.1 μM。GDC-0068处理LNCaP, PC3 和 BT474M1 细胞,抑制Akt底物PRAS40磷酸化,IC50分别为157 nM, 197 nM, 和208 nM。而且, GDC-0068选择性抑制细胞周期进展和Akt信号驱动的癌细胞活力, 包括肿瘤抑制基因PTEN缺陷,PIK3CA致癌基因突变, 和HER2扩增,在HER2+和Luminal 亚型中作用效果最强。[1-4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCC70  NXu0XYx2TnWwY4Tpc44hSXO|YYm= M3;NSVEh|ryP NUW1SZl7OjRiaB?= MkfabY5kemWjc3XzJJRp\SCjYoXu[IFv[2Vib3[gTGVTOyCjbnSgbY5lfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJEhi[3SrdnH0bY9vMSCxZjDic5RpKEWJRmKgZY5lKEiHUkO= M3zLUlI1PjZ5M{e2
MDA-MB-468  NF;EPJRHfW6ldHnvckBCe3OjeR?= M1HJU|Eh|ryP M4PBUVI1KGh? M1;YUolv[3KnYYPld{B1cGViYXL1coRidmOnIH;mJGhGWjN? NHfMNFgzPDZ4N{O3Oi=>
HCC70  M{jlZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLVT4wyKM7:TR?= MoTOOUBl M1vvZoVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SC{ZYPwc45{\Q>? MnX2NlQ3Pjd|N{[=
MDA-MB-468  NE\xRWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTEeYoyKM7:TR?= NYCyT5d6PSCm MVXlcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUhemW|cH;ud4U> NFeydHczPDZ4N{O3Oi=>
PC-3 NX;ycFVbTnWwY4Tpc44hSXO|YYm= MlzCNE4xODN6LUKuOUDPxE1? Mo\HNUBp MmTXSG1UVw>? MUfpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gRYt1KHCqb4PwbI9zgWyjdHnvckBifCCkb4ToJHRpejNyONMgLHQ{ODhrIHHu[EBU\XJ2N{O= MmD4NlMzQDd3NkO=
BT474M1 MX\GeY5kfGmxbjDBd5NigQ>? M3nmfFAvODB|OD2yMlUh|ryP M2K3N|EhcA>? MXLEUXNQ NV3pWXU3cW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgZo91cCCWaIKzNFjDqCiWM{C4LUBidmRiU3XyOFc{ NHXQcXQzOzJ6N{W2Ny=>
IGROV-1 MoLmSpVv[3Srb36gRZN{[Xl? NHzi[YwxNjByM{itNk42KM7:TR?= NFWxc2QyKGh? MYXEUXNQ M13BSYlv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBCc3RicHjvd5Bpd3K7bHH0bY9vKGG2IHLveIghXGi{M{C4xsApXDNyODmgZY5lKFOnckS3Ny=> MmjjNlMzQDd3NkO=
PC-3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHZNJcyNzVxMUCg{txO NWW0SZluOjRxNEivO|IhcA>? M{[xc2ROW09? M1;IUYRwe2VvZHXw[Y5l\W62bImgbY5kemWjc3XzJJRp\SCJMPMAl2cyyqCyaHHz[UBxd3C3bHH0bY9vyqB? MnXrNlMzQDd3NkO=
MCF7-neo/HER2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYGxM|UwOTBizszN MlXuNlQwPDhxN{KgbC=> NGm5UYJFVVOR M3PuUYRwe2VvZHXw[Y5l\W62bImgbY5kemWjc3XzJJRp\SCJMPMAl2cyyqCyaHHz[UBxd3C3bHH0bY9vyqB? NXHuR4w4OjN{OEe1OlM>
BT474M1 NFXiVHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfuZ20yNzVxMUCg{txO MnfXNlQwPDhxN{KgbC=> MYPEUXNQ MYHkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh M17Mc|I{Ojh5NU[z
PC-3 NETic2RCeG:ydH;zbZMhSXO|YYm= M1XTcFEwPS9zMDFOwG0> MmLxNVUwPDhxN{KgbC=> M4rvOWROW09? MWXjZZV{\XNiYTDkc5NmNSCjbnSgeIlu\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gZZBweHSxdHnjJIFv\CCwZXPyc5Rq[yCyb4D1cIF1cW:wcx?= MmPJNlMzQDd3NkO=
MCF7-neo/HER2 M2K1S2Fxd3C2b4Ppd{BCe3OjeR?= MnHtNU82NzFyIN88US=> NFXOeYIyPS92OD:3NkBp MVvEUXNQ M2HnOINifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z MoLrNlMzQDd3NkO=
BT474M1 NV3BbVIySXCxcITvd4l{KEG|c3H5 MonSNU82NzFyIN88US=> MX2xOU81QC95MjDo MnjrSG1UVw>? NV[wT4di[2G3c3XzJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JIlv[3KnYYPlJIlvKGGyb4D0c5Rq[yCjbnSgcoVkem:2aXOgdI9xfWyjdHnvcpM> MnHzNlMzQDd3NkO=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PUMA ; 

PubMed: 30185800     


Western blotting analysis of PUMA expression in various colon cancer cell lines treated with 10 μM ipatasertib for 24 h.

p-AKT / AKT / p-FoxO3a / FoxO3a / p-p65 / p65 ; 

PubMed: 30185800     


The expressions of P-Akt (S473), P-FoxO3a (S253), P-p65(S536), and PUMA were detected after the treatment of 10 μM ipatasertib in HCT116 at 0, 6, 12, and 24 h after 10 μM ipatasertib treatment. 

Noxa / Bid / Bad / Bim / Bcl-2 / Bcl-xl / Mcl-1; 

PubMed: 30185800     


Noxa, Bid, Bad, Bim, Bcl-2, Bcl-XL, Mcl-1 were detected in HCT-116 cells after ipatasertib for 24 h. 

cleaved-caspase3; 

PubMed: 30185800     


(a, c, e) Western blotting analysis of PUMA and C-Caspase3 expression after the treatment of 10 μM ipatasertib in combination with (a) 20 mg/ml 5-FU or (c) 40 μM Cisplatin or (e) 20 mM Regorafenib alone, or their combinations for 24 h in HCT116. 

p-PRAS40(T246) / PRAS40 / p-ERK / ERK / pFOXO1 / pFOXO3a / pGSK3b(S9) / pAS160(S318) / pBAD(S136) / pS6 / p4E-BP1; 

PubMed: 26469692     


MDA-MB 453 breast cancer cell line (PIK3CAH1047R; Her2 amp) were treated with various concentrations (1 = 0, 2 = 0.012, 3 = 0.037, 4 = 0.11, 5 = 0.33, and 6 = 1 μM) of ARQ 092, ARQ 751, MK-2206 or GDC-0068 for 2 hours. pAKT(S473), pAKT(T308), pPRAS40(T246), pFOXO1(T24) /3a(T36), pGSK3β(S9), pAS160(S318), pBAD(S136), pS6(S235/236) and p4E-BP1(S65) and phospho ERK were assessed by western blot analysis.

30185800 26469692
体内研究 GDC-0068口服处理给药PC3前列腺移植瘤模型,诱导p-PRAS40下调。GDC-0068 处理BT474-Tr移植瘤,降低 pS6 和 peIF4G 水平,重新定位FOXO3a到细胞核,且诱导 HER3 和pERK的反馈上调。GDC-0068 处理多种移植瘤模型,具有有效抗癌活性,包括PTEN-缺陷的前列腺癌模型LNCaP 和 PC3, PIK3CA H1047R 突变的乳腺癌模型 KPL-4, 和 MCF7-neo/HER2肿瘤模型。[1-4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:[1]
+ 展开
  • Animal Models: 携带LNCaP, PC3, KPL-4, 或MCF7移植瘤的雌性裸鼠
  • Formulation: 在0.5% 甲基纤维素/0.2% Tween-80中配制
  • Dosages: ~100 mg/kg/day
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 92 mg/mL (200.87 mM)
Ethanol 92 mg/mL (200.87 mM)
Water Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 458
化学式

C24H32ClN5O2

CAS号 1001264-89-6
稳定性 powder
in solvent
别名 RG7440

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01896531 Active not recruiting Gastric Cancer Genentech Inc. August 31 2013 Phase 2
NCT01896531 Active not recruiting Gastric Cancer Genentech Inc. August 31 2013 Phase 2
NCT01090960 Completed Solid Cancers Genentech Inc. March 2010 Phase 1
NCT01090960 Completed Solid Cancers Genentech Inc. March 2010 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID