Ipatasertib (Synonyms: GDC-0068; RG7440)

目录号: HY-15186 纯度: 99.79%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Ipatasertib (GDC-0068) 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 Chemical Structure

CAS No. : 1001264-89-6

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3. 试用装只面向终端客户。

规格	价格	是否有货
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	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Ipatasertib:

MCE 顾客使用本产品发表的 39 篇科研文献

: 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.

Ipatasertib 相关产品

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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) 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)

细胞效力
(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]

体外研究
(In Vitro)

Ipatasertib (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 (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 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 (10 µM; 24 h) 通过 PUMA/Bax 途径诱导 HCT116 细胞凋亡^[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.

体内研究
(In Vivo)

Ipatasertib (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.

Clinical Trial

分子量

458.00

Formula

C₂₄H₃₂ClN₅O₂

CAS 号

1001264-89-6

性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (218.34 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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

配制储备液

浓度溶剂体积质量	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
10 mM	0.2183 mL	1.0917 mL	2.1834 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (10.92 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (10.92 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.54 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 0.5% Methyl cellulose/0.5% Tween-80 in Saline water
Solubility: 10 mg/mL (21.83 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.88%

选择批次：

Data Sheet (644 KB) SDS (393 KB)

COA (290 KB) HNMR (258 KB) RP-HPLC (294 KB) MS (82 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Sun L, et al. Ipatasertib, a novel Akt inhibitor, induces transcription factor FoxO3a and NF-κB directly regulates PUMA-dependent apoptosis. Cell Death Dis. 2018 Sep 5;9(9):911. [Content Brief]

[2]. Blake JF, 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. [Content Brief]

Ipatasertib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.1834 mL	10.9170 mL	21.8341 mL	54.5852 mL
H₂O / DMSO	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

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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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Ipatasertib (Synonyms: GDC-0068; RG7440)

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Other Forms of Ipatasertib:

MCE 顾客使用本产品发表的 39 篇科研文献

Ipatasertib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Akt 亚型特异性产品:

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纯度 & 产品资料

参考文献

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Ipatasertib 相关分类

完整储备液配制表

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Ipatasertib (Synonyms: GDC-0068; RG7440)

Customer Review

Other Forms of Ipatasertib:

Ipatasertib 相关抗体

MCE 顾客使用本产品发表的 39 篇科研文献

Ipatasertib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Akt 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Ipatasertib 相关抗体:

摩尔计算器

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完整储备液配制表

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