Gedatolisib (Synonyms: PKI-587; PF-05212384)

目录号: HY-10681 纯度: 99.68%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

Gedatolisib (PKI-587) 是一种高效的双重 PI3Kα，PI3Kγ 和 mTOR 抑制剂, IC₅₀ 分别为 0.4 nM，5.4 nM 和 1.6 nM。Gedatolisib 在 mTOR 复合物 mTORC1 和 mTORC2 中同样有效。

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Gedatolisib Chemical Structure

CAS No. : 1197160-78-3

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5 mg	￥580	In-stock
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100 mg	￥5800	In-stock
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Customer Review

MCE 顾客使用本产品发表的 4 篇科研文献

Gedatolisib 相关产品

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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mTOR mTORC1 mTORC2

生物活性
纯度 & 产品资料
参考文献

生物活性

Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC₅₀s of 0.4 nM, 5.4 nM and 1.6 nM, respectively^[1]. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2^[2].

IC₅₀ & Target^[1]^[3]

PI3Kα

0.4 nM (IC₅₀)

PI3Kα-H1047R

0.6 nM (IC₅₀)

PI3Kα-E545K

0.6 nM (IC₅₀)

PI3Kγ

5.4 nM (IC₅₀)

PI3Kβ

6 nM (IC₅₀)

PI3Kδ

6 nM (IC₅₀)

mTOR

1.6 nM (IC₅₀)

mTORC1

mTORC2

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.06 μM Compound: 6aa	Antiproliferative activity against human A431 cells harboring wild type EGFR mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A431 cells harboring wild type EGFR mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34971874]
BaF3	IC₅₀	0.1 μM Compound: 6aa	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34971874]
CNE-2	IC₅₀	0.2 μM Compound: 6aa	Antiproliferative activity against human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
HCT-116	IC₅₀	0.51 μM Compound: 6aa	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
HeLa	IC₅₀	5.51 μM Compound: 6aa	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
HepG2	IC₅₀	14.76 μM Compound: 6aa	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
L02	IC₅₀	27.33 μM Compound: 6aa	Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
MCF7	IC₅₀	0.37 μM Compound: 6aa	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
MDA-MB-231	IC₅₀	1.08 μM Compound: 6aa	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
MDA-MB-361	IC₅₀	< 10 nM Compound: 26, PKI-587	Inhibition of Akt S473 phosphorylation in human MDA-MB-361 cells by Western blotting Inhibition of Akt S473 phosphorylation in human MDA-MB-361 cells by Western blotting	[PMID: 20166697]
MDA-MB-361	IC₅₀	3 nM Compound: 1, PKI-587	Growth inhibition of human MDA-MB-361 cells after 72 hrs Growth inhibition of human MDA-MB-361 cells after 72 hrs	[PMID: 21763134]
MDA-MB-361	IC₅₀	8 nM Compound: 26, PKI-587	Inhibition of Akt T308 phosphorylation in human MDA-MB-361 cells by Western blotting Inhibition of Akt T308 phosphorylation in human MDA-MB-361 cells by Western blotting	[PMID: 20166697]
NCI-H1975	IC₅₀	0.115 μM Compound: 6aa	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34971874]
PC-3	IC₅₀	11 nM Compound: 1, PKI-587	Growth inhibition of human PC3 cells after 72 hrs Growth inhibition of human PC3 cells after 72 hrs	[PMID: 21763134]
Sf9	IC₅₀	0.4 nM Compound: 1, PKI-587	Inhibition of human PI3Kalpha expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay Inhibition of human PI3Kalpha expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay	[PMID: 21763134]
Sf9	IC₅₀	11 nM Compound: 1, PKI-587	Inhibition of human PI3Kgamma expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay Inhibition of human PI3Kgamma expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay	[PMID: 21763134]

体外研究
(In Vitro)

Gedatolisib (PKI-587) 在使用 MDA-361 和 PC3-MM2 细胞系的细胞生长抑制试验中表现出良好的效力，IC₅₀ 分别为 4.0 和 13.1 nM^[1]。
Gedatolisib 可有效抑制 MDA-361 肿瘤细胞中 PI3K/mTOR 信号通路蛋白的磷酸化。Gedatolisib (0.03-3 μM；4 小时) 阻止 Akt 在 Thr 308 处的磷酸化并在 30 nM 诱导裂解的 PARP^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	MDA-361 tumor cells
Concentration:	0.03, 0.1, 0.3, 1, and 3 μM
Incubation Time:	4 hours
Result:	Prevented the phosphorylation of Akt (pAkt) at threonine 308 (T308; IC₅₀=8 nM).

体内研究
(In Vivo)

Gedatolisib（PKI-587；在第 1、5、9 天以 20 mg/kg 静脉注射）对小鼠 MDA-361 肿瘤表现出有效的抗肿瘤功效^[1]。
由于高血浆清除率 (7 mL/min/kg) 和静脉注射后的大分布体积 (分别为 7.2 L/kg)，Gedatolisib 表现出最终消除半衰期 (T_1/2 14.4 h)。给药（25 mg/kg）雌性裸鼠^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nude mice bearing MDA-361 xenograft model^[1].
Dosage:	20 mg/kg
Administration:	Administered i.v. at 20 mg/kg on an intermittent regimen (days 1, 5, 9).
Result:	Caused regression of large staged (~900 mm³) tumors. The minimum efficacious dose (MED) was determined to be 3 mg/kg against MDA-361 tumors and maximum tolerated single dose (MTD) was determined to be 30 mg/kg.

Clinical Trial

分子量

615.73

Formula

C₃₂H₄₁N₉O₄

CAS 号

1197160-78-3

性状

固体

颜色

White to off-white

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	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 4 mg/mL (6.50 mM; 加热助溶; 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 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6241 mL	8.1204 mL	16.2409 mL
5 mM	0.3248 mL	1.6241 mL	3.2482 mL
10 mM	---	---	---

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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

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

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.68%

选择批次：

Data Sheet (619 KB) SDS (393 KB)

COA (261 KB) LCMS (122 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Venkatesan AM, et al. Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J Med Chem. 2010, 53(6), 2636-2645. [Content Brief]

[2]. Freitag H, et al. Inhibition of mTOR's Catalytic Site by PKI-587 Is a Promising Therapeutic Option for Gastroenteropancreatic Neuroendocrine Tumor Disease. Neuroendocrinology. 2017;105(1):90-104. [Content Brief]

Gedatolisib 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

DMSO	1 mM	1.6241 mL	8.1204 mL	16.2409 mL	40.6022 mL
DMSO	5 mM	0.3248 mL	1.6241 mL	3.2482 mL	8.1204 mL

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.

Keywords:

Gedatolisib1197160-78-3PKI-587 PF-05212384PKI587PKI 587PF05212384PF 05212384PF-05212384PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Gedatolisib (Synonyms: PKI-587; PF-05212384)

Customer Review

MCE 顾客使用本产品发表的 4 篇科研文献