PI-103

目录号: HY-10115 纯度: 98.93%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

PI-103 是一种有效的 PI3K 和 mTOR 抑制剂，抑制 p110α，p110β，p110δ，p110γ，mTORC1 和 mTORC2，IC₅₀ 分别为 8 nM，88 nM，48 nM，150 nM，20 nM 和 83 nM。PI-103 还抑制 DNA-PK，IC₅₀ 为 2 nM。PI-103 诱导自噬 (autophagy)。

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PI-103 Chemical Structure

CAS No. : 371935-74-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1089	In-stock
1 mg	￥450	In-stock
5 mg	￥990	In-stock
10 mg	￥1550	In-stock
50 mg	￥3464	In-stock
100 mg	￥4201	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

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Customer Review

Other Forms of PI-103:

PI-103 Hydrochloride In-stock

MCE 顾客使用本产品发表的 23 篇科研文献

PI-103 相关产品

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•同靶点蛋白产品:

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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
实验参考方法
纯度 & 产品资料
参考文献

生物活性

PI-103 is a potent PI3K and mTOR inhibitor with IC₅₀s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy^[1]^[2]^[3]^[4].

IC₅₀ & Target^[1]^[4]

p110α

8 nM (IC₅₀)

p110β

88 nM (IC₅₀)

p110δ

48 nM (IC₅₀)

p110γ

150 nM (IC₅₀)

PI3KC2β

26 nM (IC₅₀)

PI3KC2α

1 μM (IC₅₀)

hsVPS34

2.3 μM (IC₅₀)

mTORC1

20 nM (IC₅₀)

mTORC2

83 nM (IC₅₀)

DNA-PK

2 nM (IC₅₀)

ATR

850 nM (IC₅₀)

ATM

920 nM (IC₅₀)

PI4KIIIβ

50 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.18 μM Compound: 7; PI-103	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
A549	IC₅₀	4 μM Compound: PI-103	Cytotoxicity against human A549 cells measured after 48 hrs by MTT assay Cytotoxicity against human A549 cells measured after 48 hrs by MTT assay	[PMID: 28011424]
Caco-2	IC₅₀	0.8 μM Compound: Pi103	Antiproliferative activity against human Caco2 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human Caco2 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
Caco-2	IC₅₀	0.9 μM Compound: PI-103	Antiproliferative activity against human Caco2 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human Caco2 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
Caco-2	IC₅₀	2 μM Compound: PI-103	Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
CWR22R	IC₅₀	0.1 μM Compound: 7; PI-103	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
Fibroblast	IC₅₀	> 20 μM Compound: PI-103	Cytotoxicity against human fibroblasts assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human fibroblasts assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
Fibroblast	IC₅₀	> 25 μM Compound: Pi103	Antiproliferative activity against human fibroblast cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human fibroblast cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
HaCaT	IC₅₀	2 μM Compound: Pi103	Antiproliferative activity against human HaCaT cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human HaCaT cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
HaCaT	IC₅₀	3.5 μM Compound: PI-103	Cytotoxicity against human HaCaT cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human HaCaT cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
HCT-116	IC₅₀	1 μM Compound: PI-103	Antiproliferative activity against human HCT116 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human HCT116 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
HCT-116	IC₅₀	3 μM Compound: Pi103	Antiproliferative activity against human HCT116 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human HCT116 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
HCT-116	IC₅₀	3.9 μM Compound: PI-103	Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
HCT-15	IC₅₀	1.76 μM Compound: PI-103	Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
HeLa	IC₅₀	0.16 μM Compound: 7; PI-103	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
HeLa	IC₅₀	3.72 μM Compound: PI-103	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
HepG2	IC₅₀	8 μM Compound: PI-103	Cytotoxicity against human HepG2 cells measured after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells measured after 48 hrs by MTT assay	[PMID: 28011424]
HT-29	IC₅₀	1.31 μM Compound: PI-103	Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
Huh-7	IC₅₀	> 20 μM Compound: PI-103	Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
Huh-7	IC₅₀	1.5 μM Compound: PI-103	Antiproliferative activity against human HuH7 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human HuH7 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
Huh-7	IC₅₀	6 μM Compound: Pi103	Antiproliferative activity against human HuH7 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human HuH7 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
HUVEC	IC₅₀	0.6 nM Compound: PI-103	Antiangiogenic activity against HUVEC after 24 hrs by calcein AM staining-based fluorescent microscopy Antiangiogenic activity against HUVEC after 24 hrs by calcein AM staining-based fluorescent microscopy	[PMID: 18849971]
MCF7	IC₅₀	13.3 μM Compound: PI-103	Cytotoxicity against human MCF7 assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human MCF7 assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
MCF7	IC₅₀	3 μM Compound: PI-103	Cytotoxicity against human MCF7 cells measured after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells measured after 48 hrs by MTT assay	[PMID: 28011424]
MDA-MB-231	IC₅₀	> 20 μM Compound: PI-103	Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
MDA-MB-231	IC₅₀	0.14 μM Compound: 7; PI-103	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
MDA-MB-231	IC₅₀	15 μM Compound: PI-103	Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
MDA-MB-231	IC₅₀	8 μM Compound: Pi103	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
MIA PaCa-2	IC₅₀	6 μM Compound: PI-103	Cytotoxicity against human MIAPaCa2 cells measured after 48 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells measured after 48 hrs by MTT assay	[PMID: 28011424]
NCI-H3122	IC₅₀	2.51 μM Compound: PI-103	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
NCI-H446	IC₅₀	2.16 μM Compound: PI-103	Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
NCI-H727	IC₅₀	> 20 μM Compound: PI-103	Cytotoxicity against human NCI-H727 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human NCI-H727 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
NCI-H727	IC₅₀	> 25 μM Compound: Pi103	Antiproliferative activity against human NCI-H727 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human NCI-H727 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
NCI-H727	IC₅₀	3 μM Compound: PI-103	Antiproliferative activity against human NCI-H727 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human NCI-H727 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
PC-3	IC₅₀	0.17 μM Compound: 7; PI-103	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
PC-3	IC₅₀	1.2 μM Compound: Pi103	Antiproliferative activity against human PC3 cells after 48 hrs by Hoechst 33342 staining-based assay Antiproliferative activity against human PC3 cells after 48 hrs by Hoechst 33342 staining-based assay	[PMID: 30655216]
PC-3	IC₅₀	1.5 μM Compound: PI-103	Antiproliferative activity against human PC3 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay Antiproliferative activity against human PC3 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay	[PMID: 23063566]
PC-3	IC₅₀	7.6 μM Compound: PI-103	Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
RL	IC₅₀	2.9 μM Compound: PI-103	Cytotoxicity against human RL assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human RL assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
Sf9	IC₅₀	1034.4 nM Compound: PI103	Inhibition of GST-tagged full length human PI3Kalpha M772A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay Inhibition of GST-tagged full length human PI3Kalpha M772A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay	[PMID: 24900786]
Sf9	IC₅₀	17.9 nM Compound: PI103	Inhibition of N-terminal His-6-tagged full length human PI3Kalpha expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay Inhibition of N-terminal His-6-tagged full length human PI3Kalpha expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay	[PMID: 24900786]
Sf9	IC₅₀	74 nM Compound: PI103	Inhibition of GST-tagged full length human PI3Kalpha D810A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay Inhibition of GST-tagged full length human PI3Kalpha D810A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay	[PMID: 24900786]
Sf9	IC₅₀	796.3 nM Compound: PI103	Inhibition of GST-tagged full length human PI3Kalpha Y836A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay Inhibition of GST-tagged full length human PI3Kalpha Y836A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay	[PMID: 24900786]
SK-OV-3	IC₅₀	0.11 μM Compound: 7; PI-103	Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method	[PMID: 32527558]
SW-620	IC₅₀	1.07 μM Compound: PI-103	Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
TT	IC₅₀	2.2 nM Compound: PI-103	Antiproliferative activity against human TT cells after 13 days by fluorescence assay Antiproliferative activity against human TT cells after 13 days by fluorescence assay	[PMID: 18849971]

体外研究
(In Vitro)

PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines^[1]. PI-103 is essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase. In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells ^[2]. PI-103 potently inhibits both the rapamycin-sensitive (mTORC1, IC₅₀=20 nM) and rapamycin-insensitive (mTORC2, IC₅₀=83 nM) complexes of the protein kinase mTOR^[4].

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

体内研究
(In Vivo)

PI-103 shows therapeutic activity against a range of human tumor xenografts, exhibiting inhibition of angiogenesis, invasion, and metastasis, as well as direct antiproliferative effects^[1]. PI-103 induces immunosuppression promoting in vivo tumor growth and inhibiting apoptosis. Tumors from PI-103-treated mice shows higher levels of cyclin D1 and more proliferating cells^[3].

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

分子量

348.36

Formula

C₁₉H₁₆N₄O₃

CAS 号

371935-74-9

性状

固体

颜色

Light yellow to green 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	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 10 mg/mL (28.71 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)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8706 mL	14.3530 mL	28.7059 mL
5 mM	0.5741 mL	2.8706 mL	5.7412 mL
10 mM	0.2871 mL	1.4353 mL	2.8706 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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: ≥ 1.05 mg/mL (3.01 mM); 澄清溶液

此方案可获得 ≥ 1.05 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.5 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% Corn Oil
Solubility: ≥ 1.05 mg/mL (3.01 mM); 澄清溶液

此方案可获得 ≥ 1.05 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 10.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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: 98.93%

选择批次：

Data Sheet (636 KB) SDS (393 KB)

COA (200 KB) HNMR (192 KB) LCMS (478 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Raynaud FI, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103through PI-540, PI-620 to the oral agent GDC-0941. Mol Cancer Ther. 2009 Jul;8(7):1725-39. [Content Brief]

[2]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110 alpha. Cell. 2006 May 19;125(4):733-47. [Content Brief]

[3]. Park S, et al. PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase anLeukemia. 2008 Sep;22(9):1698-706.d mTOR, has antileukemicactivity in AmL. Leukemia. 2008 Sep;22(9):1698-706. [Content Brief]

[4]. López-Fauqued M, et al. The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of melanoma cells. Int J Cancer. 2010 Apr 1;126(7):1549-61. [Content Brief]

Kinase Assay ^[4]	IC₅₀ values are measured using either a standard thin-layer chromatography (TLC) assay for lipid kinase activity or a high-throughput membrane capture assay. Kinase reactions are performed by preparing a reaction mixture containing kinase, inhibitor (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl₂), and freshly sonicated phosphatidylinositol (100 μg/mL). Reactions are initiated by the addition of ATP containing 10 μCi of γ-32P-ATP to a final concentration 10 or 100 μM, and allowed to proceed for 20 minutes at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 μL 1N HCl followed by 160 μL CHCl₃:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl₃. This extract is spotted on TLC plates and developed for 3-4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. For each compound, kinase activity is typically measured at 10-12 inhibitor concentrations representing two-fold dilutions from the highest concentration tested (100 μM). For compounds showing significant activity, IC₅₀ determinations are repeated two to four times, and the reported value is the average of these independent measurements^[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[2]	For proliferation assays, MOLM14, OCI-AmL3 and MV4-11 cells are cultured during 48 h at 10⁵ cells/mL, in triplicate, in 10% FCS, without or with 0.1 or 1 μM PI-103, and then pulsed 6 h with 1μCi (37 kBq) [⁴H]-thymidine. The amounts oadioactivity are determined after trichloracetic acid precipitation^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] Five to six month old males of either FVB/N strain or nude BALB/c strain are injected subcutaneously with one million cells in PBS. When tumor reaches between 50 and 100 mm³, mice are treated with 10 mg/kg or 70 mg/kg of PI-103 by IP injection daily. Control mice are treated with the same volume of DMSO. Tumor size and mice weight is monitored every 2 days. When mice are sacrificed, tumors are dissected and processed^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Raynaud FI, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103through PI-540, PI-620 to the oral agent GDC-0941. Mol Cancer Ther. 2009 Jul;8(7):1725-39. [Content Brief] [2]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110 alpha. Cell. 2006 May 19;125(4):733-47. [Content Brief] [3]. Park S, et al. PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase anLeukemia. 2008 Sep;22(9):1698-706.d mTOR, has antileukemicactivity in AmL. Leukemia. 2008 Sep;22(9):1698-706. [Content Brief] [4]. López-Fauqued M, et al. The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of melanoma cells. Int J Cancer. 2010 Apr 1;126(7):1549-61. [Content Brief]

PI-103 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	2.8706 mL	14.3530 mL	28.7059 mL	71.7648 mL
	5 mM	0.5741 mL	2.8706 mL	5.7412 mL	14.3530 mL
	10 mM	0.2871 mL	1.4353 mL	2.8706 mL	7.1765 mL
	15 mM	0.1914 mL	0.9569 mL	1.9137 mL	4.7843 mL
	20 mM	0.1435 mL	0.7176 mL	1.4353 mL	3.5882 mL
	25 mM	0.1148 mL	0.5741 mL	1.1482 mL	2.8706 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:

PI-103371935-74-9PI103PI 103PI3KmTORDNA-PKAutophagyApoptosisPhosphoinositide 3-kinaseMammalian target of RapamycinDNA-dependent protein kinaseInhibitorinhibitorinhibit

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PI-103

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