Ipatasertib (GDC-0068)

目录号：S2808 别名： RG7440

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

10mM (in 1mL DMSO)	RMB 3094.44	现货
5mg	RMB 2192.93	现货
10mg	RMB 3025.41	现货
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客户使用Selleck该产品发表文献8篇：

Nat Commun, 2018, 9(1):4550

PubMed: 30382095 ( click the link to review the publication )

Clin Cancer Res, 2018, 78(7):1657-1671

PubMed: 29358169 ( click the link to review the publication )

Leukemia, 2018, 32(1):214-223

PubMed: 28878352 ( click the link to review the publication )

Neoplasia, 2017, 19(4):310-320

PubMed: 28285180 ( click the link to review the publication )

Mol Cancer Ther, 2016, 10.1158/1535-7163.MCT-15-0748

PubMed: 27297869 ( click the link to review the publication )

Cell, 2015, 160(1-2):161-76

PubMed: 25594179 ( click the link to review the publication )

Mol Cancer Ther, 2015, 14(8):1928-38

PubMed: 25995437 ( click the link to review the publication )

J Biol Chem, 2014, 289(49):34189-204

PubMed: 25331943 ( click the link to review the publication )

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 Cell Death Dis 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 Cell Death Dis 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 Cell Death Dis 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 Cell Death Dis (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 PLoS One 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]

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)

参考文献

+ 展开

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 Download Ipatasertib (GDC-0068) SDF

分子量	458
化学式	C₂₄H₃₂ClN₅O₂
CAS号	1001264-89-6
稳定性	3 years -20°C powder
稳定性	2 years -80°C in solvent
别名	RG7440

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

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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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 (data from https://clinicaltrials.gov, updated on 2019-03-27)

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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操作手册

如果有其他问题，请给我们留言。

Akt Signaling Pathway Map

Akt Inhibitors with Unique Features

选择性强的Akt抑制剂

CCT128930 : Akt2-selective, IC50=6 nM.
活性最高的Akt抑制剂

AZD5363 : Akt1, IC50=3 nM; Akt2, IC50=8 nM; Akt3, IC50=8 nM.
用于临床的Akt抑制剂

Perifosine (KRX-0401) : Phase III for relapsed and refractory multiple myeloma.
最新的Akt抑制剂

AZD5363 : Potent inhibitor of all isoforms of Akt (Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM, similar to P70S6K/PKA and lower activity towards ROCK1/2.

研究领域

产品类型

Ipatasertib (GDC-0068)

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：

产品安全说明书

Akt抑制剂选择性比较

生物活性

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)

参考文献

溶解度 (25°C)

化学数据 Download Ipatasertib (GDC-0068) SDF

计算器

摩尔浓度计算器

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

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2019-03-27)

技术支持

Akt Signaling Pathway Map

Akt Inhibitors with Unique Features

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