Ipatasertib | GDC-0068 | Pan-Akt Inhibitor | AmBeed-信号通路专用抑制剂

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Ipatasertib 99%+

货号：A115731 同义名： GDC-0068;RG7440

Ipatasertib (GDC-0068) 是一种口服活性、高度选择性和 ATP 竞争性的泛-Akt 抑制剂，对 Akt1/2/3 的 IC50 值分别为 5、18 和 8 nM。通过 Akt 抑制同步激活 FOXO3a 和 NF-κB，导致 PUMA 的 p53 独立激活。Ipatasertib 在癌细胞中诱导凋亡并抑制异种移植小鼠模型中的肿瘤生长。

Ipatasertib 化学结构
CAS号：1001264-89-6

Ipatasertib 3D分子结构
CAS号：1001264-89-6

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Ipatasertib 纯度/质量文件产品仅供科研

货号：A115731 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

Akt 亚型比较

产品名称	Akt ↓ ↑	Akt1 ↓ ↑	Akt2 ↓ ↑	Akt3 ↓ ↑	其他靶点	纯度
Honokiol	✔				MEK	98%
PF-04691502	++++ P-Akt (T308), IC50: 7.5 nM P-Akt (S473), IC50: 3.8 nM					98+%
PHT-427	+ Akt, Ki: 2.7 μM					99%+
Deguelin	✔				PI3K	99%+
TIC10 isomer	✔				ERK	98+%
Perifosine	+ Akt, IC50: 4.7 μM					98%
Miltefosine	✔				PI3K,PKC	98%
Triciribine	+ Akt, IC50: 130 nM					99%+
Uprosertib		+ Akt1, IC50: 180 nM	+ Akt2, IC50: 328 nM	++ Akt3, IC50: 38 nM		99%+
Afuresertib		++++ Akt1, Ki: 0.08 nM	++++ Akt2, Ki: 2 nM	++++ Akt3, Ki: 2.6 nM		99%+
Miransertib		++++ Akt1, IC50: 5 nM	++++ Akt2, IC50: 4.5 nM	++ Akt3, IC50: 16 nM		98+%
GSK-690693		++++ Akt1, IC50: 2 nM	+++ Akt2, IC50: 13 nM	+++ Akt3, IC50: 9 nM		99%+
AT7867		++ Akt1, IC50: 32 nM	++ Akt2, IC50: 17 nM	++ Akt3, IC50: 47 nM	PKA	99%+
AKT inhibitor VIII		++ Akt1, IC50: 58 nM	+ Akt2, IC50: 210 nM	+ Akt3, IC50: 2119 nM		98+%
MK-2206 2HCl		+++ Akt1, IC50: 8 nM	+++ Akt2, IC50: 12 nM	+ Akt3, IC50: 65 nM		99%+
Ipatasertib		++++ Akt1, IC50: 5 nM	++ Akt2, IC50: 18 nM	+++ Akt3, IC50: 8 nM		99%+
AT13148		++ Akt1, IC50: 38 nM	+ Akt2, IC50: 402 nM	++ Akt3, IC50: 50 nM	PKA	98+%
Capivasertib		++++ Akt1, IC50: 3 nM	+++ Akt2, IC50: 8 nM	+++ Akt3, IC50: 8 nM		99%+
A-674563 HCl		+++ Akt1, Ki: 11 nM			PKA	98%
CCT128930			+++ Akt2, IC50: 6 nM		PKA	98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Ipatasertib 生物活性

靶点	Akt3 Akt3, IC50:8 nM Akt1 Akt1, IC50:5 nM Akt2 Akt2, IC50:18 nM
描述	AKT is the central node of PI3K/AKT/mTOR pathway. The PH domain and ATP-competitive site are the main target site for research of new compound^[1]. GDC-0068 (Ipatasertib) is an ATP-competitive pan Akt inhibitor with IC50 values of 5 nM, 18 nM and 8 nM on AKT 1, 2 and 3 isoforms, respectively^[2]. Treatment of GDC-0068 on concentration of 0.1 - 25 μM caused decreased phosphorylation of the downstream targets of AKT, such as FoxO1 and FoxO3a, 4EBP1 and S6 in a dose- and time-dependent manner in PC-3, BT474M1, and IGROV-1 cell lines, accompanied by feedback increase in AKT phosphorylation. Treatment of GDC-0068 on concentration of 1 – 10 μM can induce G1-arrest (including in PC-3 cells) and increase in apoptotic and necrotic populations in a dose- and time-dependent manner in BT474M1 and MCF7-neo/HER2 cells, but not in PC-3 cells. In growth inhibition assay, cell lines with high Akt activity show more sensitivity to GDC-0068. GDC-0068 showed good pharmacokinetics and pharmacodynamics in xenograft models. The level of pPRAS40-T246 in LNCaP tumors at 1 and 4 hours after a single dose of GDC-0068 at 12.5, 25, 50, or 100 mg/kg decreased in a dose-dependent manner. GDC-0068 on dose of 50 mg/kg in combination with docetaxel induced tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models^[3]. The clinical trials of GDC-0068, including a completed phase 2 study of combination with paclitaxel as neoadjuvant treatment for participants with early stage triple negative breast cancer, have been done (see in https://clinicaltrials.gov/).
作用机制	GDC-0068 is an ATP-competitive AKT inhibitor.

Ipatasertib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
BT474M1	0.0038-2.5 μM	Function Assay	1 h	induces a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser473	23287563
BT474M1	1/5/10 μM	Growth Inhibition Assay	24/48/72 h	dose-dependently increases the G0–G1 phase population	23287563
BT474M1	1/5/10 μM	Apoptosis Assay	15/48/72 h	causes a dose- and time-dependent increase in apoptotic and necrotic populations	23287563
HCC70	1 μM	Function Assay	24 h	increases the abundance of HER3 and induces the phosphorylation (activation) of both EGFR and HER3	24667376

Ipatasertib 动物研究

Dose

Mice: min = 40 mg/kg^[4] (s.c.), max = 100 mg/kg^[3] (p.o.)

Administration

s.c., p.o.

Pharmacokinetics

Animal	Mice^[3]
C_max	4-8 h

Ipatasertib 参考文献

[1]Huck BR, Mochalkin I, et al. Recent progress towards clinically relevant ATP-competitive Akt inhibitors. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2838-2848.

[2]Blake JF, Xu R, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27. Epub 2012 Sep 18.

[3]Lin J, Sampath D, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72.

[4]EP2928488A1

Ipatasertib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.92mL

2.18mL

1.09mL

21.83mL

4.37mL

2.18mL

Ipatasertib 技术信息

CAS号	1001264-89-6
分子式	C₂₄H₃₂ClN₅O₂
分子量	457.996

别名	GDC-0068;RG7440
运输	蓝冰

存储条件

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 200 mg/mL(436.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 3 mg/mL(6.55 mM)，配合低频超声，并水浴加热至45℃助溶

动物实验配方

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

BT474M1	0.0038-2.5 μM	Function Assay	1 h	induces a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser473	23287563
BT474M1	1/5/10 μM	Growth Inhibition Assay	24/48/72 h	dose-dependently increases the G0–G1 phase population	23287563
BT474M1	1/5/10 μM	Apoptosis Assay	15/48/72 h	causes a dose- and time-dependent increase in apoptotic and necrotic populations	23287563
HCC70	1 μM	Function Assay	24 h	increases the abundance of HER3 and induces the phosphorylation (activation) of both EGFR and HER3	24667376
HCC70	1 μM	Growth Inhibition Assay	5 d	enhances the antiproliferative response	24667376
IGROV-1	0.0038-2.5 μM	Function Assay	1 h	induces a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser473	23287563
MCF7-neo/HER2	1/5/10 μM	Growth Inhibition Assay	24/48/72 h	dose-dependently increases the G0–G1 phase population	23287563
MCF7-neo/HER2	1/5/10 μM	Apoptosis Assay	15/48/72 h	causes a dose- and time-dependent increase in apoptotic and necrotic populations	23287563
MDA-MB-468	1 μM	Function Assay	24 h	increases the abundance of HER3	24667376
MDA-MB-468	1 μM	Growth Inhibition Assay	5 d	enhances the antiproliferative response	24667376
PC-3	0.0038-2.5 μM	Function Assay	1 h	induces a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser473	23287563
PC-3	1/5/10 μM	Growth Inhibition Assay	24/48/72 h	dose-dependently increases the G0–G1 phase population	23287563
PC-3	1/5/10 μM	Apoptosis Assay	15/48/72 h	causes a dose- and time-dependent increase in apoptotic and necrotic populations	23287563

Ipatasertib 99%+

Ipatasertib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Ipatasertib 质控信息

Ipatasertib 生物活性

Ipatasertib 细胞研究

Ipatasertib 动物研究

Ipatasertib 参考文献

Ipatasertib 实验方案

Ipatasertib 技术信息

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Ipatasertib 99%+

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Ipatasertib 质控信息

Ipatasertib 生物活性

Ipatasertib 细胞研究

Ipatasertib 动物研究

Ipatasertib 参考文献

Ipatasertib 实验方案

Ipatasertib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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