AZ7550

目录号: HY-B0794: Data Sheet 产品使用指南
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技术支持

AZ7550 是 AZD9291 的一种活性代谢物，AZ7550 抑制 IGF1R 活性，IC₅₀ 为 1.6 μM。

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AZ7550 Chemical Structure

CAS No. : 1421373-99-0

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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
5 mg	￥2800	In-stock
10 mg	￥4400	In-stock
25 mg	现货	询价
50 mg	现货	询价
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 AZ7550:

MCE 顾客使用本产品发表的 3 篇科研文献

AZ7550 相关产品

•相关化合物库:

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•同靶点蛋白产品:

查看 EGFR 亚型特异性产品:

查看所有亚型

EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC₅₀ of 1.6 μM.

IC₅₀ & Target

IC50: 1.6 μM (IGF1R), 88 nM (MLK1), 156 nM (ACK1), 195 nM (ErbB4), 228 nM (MNK2), 302 nM (FLT3), 420 nM (ALK ), 449 nM (FES), 840 nM (IRR), 843 nM (BRK), 977 nM (BLK), 995 nM (FAK), 1256 nM (Ins R), 1317 nM (TEC), 1784 nM (FLT4), 2288 nM (PYK2), 2443 nM (Txk), 5104 nM (BTK)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Calu-3	GI₅₀	537 nM Compound: 28	Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
LoVo	IC₅₀	786 nM Compound: AZ7550	Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA	[PMID: 26968253]
LoVo	IC₅₀	786 μM Compound: 28	Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay	[PMID: 25271963]
NCI-H1975	GI₅₀	19 nM Compound: 28	Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
NCI-H1975	IC₅₀	45 μM Compound: 28	Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 25271963]
PC-9	GI₅₀	15 nM Compound: 28	Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
PC-9	IC₅₀	26 nM Compound: AZ7550	Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA	[PMID: 26968253]
PC-9	IC₅₀	26 μM Compound: 28	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay	[PMID: 25271963]

体外研究
(In Vitro)

AZ7550 (Compound 28) appeares to offer a broadly similar potency and selectivity profile to the parent compound AZD9291. AZ7550 inhibits double mutant (DM) cell line H1975, activating mutant (AM) cell line PC9, and wild type (WT) cell line LoVo with IC₅₀s of 45, 26, and 786 nM, respectively. AZ7550 inhibits DM antiproliferative cell line H1975, AM antiproliferative cell line PC9, and WT antiproliferative cell line Calu3 with GI₅₀s of 19, 15, and 537 nM, respectively^[1].

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

Clinical Trial

分子量

485.58

Formula

C₂₇H₃₁N₇O₂

CAS 号

1421373-99-0

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 : 83.33 mg/mL (171.61 mM; ultrasonic and adjust pH to 5 with 1 M HCL; 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	2.0594 mL	10.2970 mL	20.5939 mL
5 mM	0.4119 mL	2.0594 mL	4.1188 mL
10 mM	0.2059 mL	1.0297 mL	2.0594 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, 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

产品使用指南 (1538 KB)

参考文献

[1]. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67. [Content Brief]

Kinase Assay ^[1]	Biochemical enzyme profiling of AZD9291 and active metabolites across the kinome panel (single profiling experiment representative of two independent studies). % inhibition for kinases in the ~280 kinase panel that shows greater than 60% inhibition after 1 μM treatment with AZD9291, AZ5104 or AZ7550, and follow-up IC₅₀s where tested, are shown. Kinases with a conserved cysteine in the analogous position within their catalytic domain as Cys797 in EGFR are also shown, highlighted in bold^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67. [Content Brief]

Kinase Assay
^[1]

Biochemical enzyme profiling of AZD9291 and active metabolites across the kinome panel (single profiling experiment representative of two independent studies). % inhibition for kinases in the ~280 kinase panel that shows greater than 60% inhibition after 1 μM treatment with AZD9291, AZ5104 or AZ7550, and follow-up IC₅₀s where tested, are shown. Kinases with a conserved cysteine in the analogous position within their catalytic domain as Cys797 in EGFR are also shown, highlighted in bold^[1].

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

参考文献

[1]. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67. [Content Brief]

AZ7550 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	2.0594 mL	10.2970 mL	20.5939 mL	51.4848 mL
	5 mM	0.4119 mL	2.0594 mL	4.1188 mL	10.2970 mL
	10 mM	0.2059 mL	1.0297 mL	2.0594 mL	5.1485 mL
	15 mM	0.1373 mL	0.6865 mL	1.3729 mL	3.4323 mL
	20 mM	0.1030 mL	0.5148 mL	1.0297 mL	2.5742 mL
	25 mM	0.0824 mL	0.4119 mL	0.8238 mL	2.0594 mL
	30 mM	0.0686 mL	0.3432 mL	0.6865 mL	1.7162 mL
	40 mM	0.0515 mL	0.2574 mL	0.5148 mL	1.2871 mL
	50 mM	0.0412 mL	0.2059 mL	0.4119 mL	1.0297 mL
	60 mM	0.0343 mL	0.1716 mL	0.3432 mL	0.8581 mL
	80 mM	0.0257 mL	0.1287 mL	0.2574 mL	0.6436 mL
	100 mM	0.0206 mL	0.1030 mL	0.2059 mL	0.5148 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:

AZ75501421373-99-0AZ 7550AZ-7550EGFRIGF-1RDrug MetaboliteEpidermal growth factor receptorErbB-1HER1Insulin-like growth factor-1 receptorInhibitorinhibitorinhibit

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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。

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沪(浦)应急管危经许[2021]201709(QFYS)

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AZ7550

Customer Review

Other Forms of AZ7550:

AZ7550 相关抗体

MCE 顾客使用本产品发表的 3 篇科研文献

AZ7550 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 EGFR 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

AZ7550 相关抗体:

摩尔计算器

稀释计算器

AZ7550 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

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