SU11274 (Synonyms: PKI-SU11274)

目录号: HY-12014 纯度: 98.82%: Data Sheet SDS COA 产品使用指南
FAQs
技术支持

SU11274 是一种选择性的 Met 抑制剂，IC₅₀ 值为 10 nM，对 PGDFRβ，EGFR 或 Tie2 没有抑制作用。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SU11274 Chemical Structure

CAS No. : 658084-23-2

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

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	￥1430	In-stock
1 mg	￥409	In-stock
5 mg	￥900	In-stock
10 mg	￥1300	In-stock
25 mg	￥2750	In-stock
50 mg	￥4400	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

MCE 顾客使用本产品发表的 7 篇科研文献

SU11274 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

SU11274 is a selective Met inhibitor with IC₅₀ of 10 nM, but has no effects on PGDFRβ, EGFR or Tie2.

IC₅₀ & Target

IC50: 10 nM (Met)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.53 μM Compound: 2, SU11274	Antiproliferative activity against mouse BAF3 cells expressing TPR-Met after 72 hrs in absence of IL-3 Antiproliferative activity against mouse BAF3 cells expressing TPR-Met after 72 hrs in absence of IL-3	[PMID: 21405128]
BaF3	IC₅₀	6.4 μM Compound: 2, SU11274	Antiproliferative activity against mouse BAF3 cells expressing TPR-Met after 72 hrs in presence of IL-3 Antiproliferative activity against mouse BAF3 cells expressing TPR-Met after 72 hrs in presence of IL-3	[PMID: 21405128]
BXPC-3	IC₅₀	16 μM Compound: 2, SU11274	Antiproliferative activity against human BxPC3 cells after 72 hrs Antiproliferative activity against human BxPC3 cells after 72 hrs	[PMID: 21405128]
HepG2	IC₅₀	1.561 μM Compound: SU, SU11274	Inhibition of Met-mediated tumorigenesis in HGF-stimulated human HepG2 cells assessed as impairment in anchorage-independent growth by soft agar growth assay Inhibition of Met-mediated tumorigenesis in HGF-stimulated human HepG2 cells assessed as impairment in anchorage-independent growth by soft agar growth assay	[PMID: 22138308]
MCF7	IC₅₀	6.2 μM Compound: 2, SU11274	Antiproliferative activity against human MCF7 cells after 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs	[PMID: 21405128]
MDA-MB-231	IC₅₀	11 μM Compound: 2, SU11274	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs	[PMID: 21405128]
MDCK	IC₅₀	0.152 μM Compound: SU, SU11274	Inhibition of Met-mediated scattering in HGF-stimulated human MDCK cells pre-incubated overnight prior to HGF stimulation for 24 hrs measured after 24 to 48 hrs Inhibition of Met-mediated scattering in HGF-stimulated human MDCK cells pre-incubated overnight prior to HGF stimulation for 24 hrs measured after 24 to 48 hrs	[PMID: 22138308]
MDCK	IC₅₀	0.2 μM Compound: SU11274	Inhibition of Met-triggered cell scattering in HGF-stimulated MDCK cells preincubated for overnight before HGF challenge measured after 24 to 48 hrs Inhibition of Met-triggered cell scattering in HGF-stimulated MDCK cells preincubated for overnight before HGF challenge measured after 24 to 48 hrs	[PMID: 22738633]
MKN-45	IC₅₀	1.3 μM Compound: 2, SU11274	Antiproliferative activity against human MKN45 cells after 72 hrs Antiproliferative activity against human MKN45 cells after 72 hrs	[PMID: 21405128]
NCI-H1993	IC₅₀	7.3 μM Compound: 2, SU11274	Antiproliferative activity against human NCI-H1993 cells after 72 hrs Antiproliferative activity against human NCI-H1993 cells after 72 hrs	[PMID: 21405128]
NCI-H441	IC₅₀	13 μM Compound: 2, SU11274	Antiproliferative activity against human NCI-H441 cells after 72 hrs Antiproliferative activity against human NCI-H441 cells after 72 hrs	[PMID: 21405128]
NIH3T3	IC₅₀	≥ 50 μM Compound: 2, SU11274	Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs	[PMID: 21405128]
NIH3T3	IC₅₀	2 μM Compound: 2, SU11274	Antiproliferative activity against mouse NIH/3T3 cells expressing TPR-Met after 72 hrs Antiproliferative activity against mouse NIH/3T3 cells expressing TPR-Met after 72 hrs	[PMID: 21405128]
SNU1	IC₅₀	7 μM Compound: 2, SU11274	Antiproliferative activity against human SNU1 cells after 72 hrs Antiproliferative activity against human SNU1 cells after 72 hrs	[PMID: 21405128]
SNU-5	IC₅₀	0.8 μM Compound: 2, SU11274	Antiproliferative activity against human SNU5 cells after 72 hrs Antiproliferative activity against human SNU5 cells after 72 hrs	[PMID: 21405128]

体外研究
(In Vitro)

SU11274 对 Met 的选择性比 Flk 高 50 倍以上，对其他酪氨酸激酶 (如 FGFR-1、c-src、PDGFbR 和 EGFR) 的选择性高 500 倍以上。SU11274 可抑制 PI3K 通路关键调控因子 (包括 AKT、FKHR 或 GSK3β) 的磷酸化。在没有白细胞介素 3 的情况下，SU11274 以剂量依赖性方式抑制 TPR-MET 转化的 BaF3 细胞的生长，IC₅₀ 小于 3 μM，而对其他致癌酪氨酸激酶 (包括 BCR-ABL、TEL-JAK2、TEL-ABL 和 TEL-PDGFβR) 转化的 BaF3 细胞的生长没有抑制作用。除了细胞生长外，SU11274 还能显著抑制 BaF3 的迁移。在浓度为 1 μM 和 5 μM 时，SU11274 分别可抑制 TPR-MET 细胞 44.8% 和 80% 的增殖。SU11274 可抑制 HGF 依赖性的 Met 磷酸化以及 HGF 依赖性的细胞增殖和迁移，IC₅₀ 为 1-1.5 μM。在具有功能性 Met 受体的 H69 和 H345 细胞中，SU11274 可抑制 HGF 诱导的细胞生长，IC₅₀ 分别为 3.4 μM 和 6.5 μM。SU11274 可诱导 G1 期细胞停滞，浓度为 5 μM 时，G1 期细胞从 42.4% 增加到 70.6%，浓度为 1 μM 时，可诱导 caspase 依赖性的细胞凋亡 24%^[2]。
SU11274 抑制表达 c-Met 的非小细胞肺癌 (NSCLC) 细胞的细胞活力，IC₅₀ 值为 0.8-4.4 μM，并消除肝细胞生长因子诱导的 c-Met 磷酸化及其下游信号传导^[3]。

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

分子量

568.09

同用名

PKI-SU11274

Formula

C₂₈H₃₀ClN₅O₄S

CAS 号

658084-23-2

性状

固体

颜色

White to 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 (176.03 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7603 mL	8.8014 mL	17.6028 mL
5 mM	0.3521 mL	1.7603 mL	3.5206 mL
10 mM	0.1760 mL	0.8801 mL	1.7603 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。

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: ≥ 2.5 mg/mL (4.40 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。

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: 98.82%

选择批次：

Data Sheet (650 KB) SDS (393 KB)

COA (296 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Wang X, et al. Potent and selective inhibitors of the Met [hepatocyte growth factor/scatter factor (HGF/SF) receptor] tyrosine kinase block HGF/SF-induced tumor cell growth and invasion. Mol Cancer Ther, 2003, 2(11):1085-1092. [Content Brief]

[2]. Sattler M, et al. A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase. Cancer Res, 2003, 63(17), 5462-5469. [Content Brief]

[3]. Ma PC, et al. Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer. Cancer Res, 2005, 65(4), 1479-1488. [Content Brief]

Kinase Assay ^[1]	A chimeric protein is constructed containing the cytoplasmic domain of human c-Met fused to Glutathione S-transferase (GST) and expressed in SF9 cells. The c-Met kinase GST-fusion protein is used for an ELISA-based Met biochemical assay using the random copolymer poly(Glu:Tyr) (4:1) immobilized on microtiter plates as a substrate. IC₅₀ value is determined with various concentrations of SU11274 in a buffer containing 5 μM ATP and 10 mM MnCl₂, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate. The kinase reaction is performed for 5 minutes at room temperature. The extent of substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[2]	Cells are exposed to various concentrations of SU11274 in the presence or absence of HGF for 24, 48, and 72 hours. The number of viable cells is determined using the MTT assay or trypan blue exclusion. Cell Cycle and apoptosis are measured by fluorescence-activated cell sorter analysis via propidium iodide staining and Annexin V-positive staining, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Wang X, et al. Potent and selective inhibitors of the Met [hepatocyte growth factor/scatter factor (HGF/SF) receptor] tyrosine kinase block HGF/SF-induced tumor cell growth and invasion. Mol Cancer Ther, 2003, 2(11):1085-1092. [Content Brief] [2]. Sattler M, et al. A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase. Cancer Res, 2003, 63(17), 5462-5469. [Content Brief] [3]. Ma PC, et al. Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer. Cancer Res, 2005, 65(4), 1479-1488. [Content Brief]

SU11274 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	1.7603 mL	8.8014 mL	17.6028 mL	44.0071 mL
	5 mM	0.3521 mL	1.7603 mL	3.5206 mL	8.8014 mL
	10 mM	0.1760 mL	0.8801 mL	1.7603 mL	4.4007 mL
	15 mM	0.1174 mL	0.5868 mL	1.1735 mL	2.9338 mL
	20 mM	0.0880 mL	0.4401 mL	0.8801 mL	2.2004 mL
	25 mM	0.0704 mL	0.3521 mL	0.7041 mL	1.7603 mL
	30 mM	0.0587 mL	0.2934 mL	0.5868 mL	1.4669 mL
	40 mM	0.0440 mL	0.2200 mL	0.4401 mL	1.1002 mL
	50 mM	0.0352 mL	0.1760 mL	0.3521 mL	0.8801 mL
	60 mM	0.0293 mL	0.1467 mL	0.2934 mL	0.7335 mL
	80 mM	0.0220 mL	0.1100 mL	0.2200 mL	0.5501 mL
	100 mM	0.0176 mL	0.0880 mL	0.1760 mL	0.4401 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:

SU11274658084-23-2PKI-SU11274SU 11274SU-11274c-Met/HGFRAutophagyApoptosisInhibitorinhibitorinhibit

您最近查看的产品:

产品名称：

* 需求量：

* 客户姓名：

* Email：

* 电话：

* 公司或机构名称：

留言给我们：

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）
Copyright © 2013-2025 MedChemExpress. All Rights Reserved.

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）

SU11274 (Synonyms: PKI-SU11274)

Customer Review

MCE 顾客使用本产品发表的 7 篇科研文献