WZ4002

目录号: HY-12026 纯度: 99.76%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

WZ4002是突变选择性的 EGFR 抑制剂；对EGFR^L858R，EGFR^L858R/T790M，EGFR^E746_A750，EGFR^{E746_A750/T790M} 的 IC₅₀ 值分别为2，8，3，2 nM。

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

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

WZ4002 Chemical Structure

CAS No. : 1213269-23-8

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	￥440	In-stock
5 mg	￥400	In-stock
10 mg	￥640	In-stock
50 mg	￥1950	In-stock
100 mg	￥3200	In-stock
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 8 篇科研文献

: WZ4002 purchased from MCE. Usage Cited in: Oncotarget. 2016 Oct 25;7(43):69760-69769. [Abstract]; Ibrutinib and WZ4002 inhibitory effects on EGFRY1068 auto-phosphorylation in the H1975 cell line at different time points by removal of drug after 4 h pretreatment

: WZ4002 purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22. [Abstract]; Effect of Ibrutinib on EGFR wt/mutant NSCLCs. Ibrutinib effects on wt EGFR and mutant EGFR- mediated signaling pathways. The results demonstrate that Ibrutinib potently inhibits both EGFR wt/mutant auto-phosphorylation at Y1068.

: WZ4002 purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22. [Abstract]; Effect of Ibrutinib, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.

WZ4002 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:

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

WZ4002 is a mutant selective EGFR inhibitor with IC₅₀s of 2, 8, 3 and 2 nM for EGFR^L858R, EGFR^L858R/T790M, EGFR^E746_A750 and EGFR^{E746_A750/T790M}, respectively.

IC₅₀ & Target^[1]

EGFR^L858R

2 nM (IC₅₀, Cell Assay)

EGFR^L858R/T790M

8 nM (IC₅₀, Cell Assay)

EGFR^E746_A750

3 nM (IC₅₀, Cell Assay)

EGFR^{E746_A750/T790M}

2 nM (IC₅₀, Cell Assay)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
16HBE14o-	IC₅₀	0.811 μM Compound: WZ4002	Antiproliferative activity against human 16HBE cells expressing wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human 16HBE cells expressing wild type EGFR after 72 hrs by MTT assay	[PMID: 23792318]
16HBE14o-	IC₅₀	1.355 μM Compound: 1, WZ4002	Antiproliferative activity against human 16HBE cells after 72 hrs by MTT assay Antiproliferative activity against human 16HBE cells after 72 hrs by MTT assay	[PMID: 24607591]
16HBE14o-	IC₅₀	1.355 μM Compound: 1, WZ4002	Cytotoxicity against human 16HBE14o- cells harboring wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human 16HBE14o- cells harboring wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23668441]
A-431	IC₅₀	1.042 μM Compound: 3; WZ4002	Antiproliferative activity against human A431 cells expressing wild type EGFR by MTS assay Antiproliferative activity against human A431 cells expressing wild type EGFR by MTS assay	[PMID: 26882288]
A-431	IC₅₀	1.108 μM Compound: 1, WZ4002	Antiproliferative activity against human A431 cells overexpressing WT EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells overexpressing WT EGFR after 72 hrs by MTT assay	[PMID: 24607591]
A-431	IC₅₀	1.108 μM Compound: 1, WZ4002	Cytotoxicity against human A431 cells overexpressing wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A431 cells overexpressing wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23668441]
A-431	IC₅₀	1.108 μM Compound: 1; WZ4002	Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay	[PMID: 27131639]
A-431	IC₅₀	1.115 μM Compound: WZ4002	Antiproliferative activity against human A431 cells expressing wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells expressing wild type EGFR after 72 hrs by MTT assay	[PMID: 23792318]
A-431	IC₅₀	1.244 μM Compound: WZ-4002	Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay	[PMID: 29534926]
A-431	IC₅₀	1.3 μM Compound: 1; WZ4002	Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay	[PMID: 28987609]
A-431	IC₅₀	1.39 μM Compound: 1, WZ4002	Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTS assay Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTS assay	[PMID: 22339342]
A-431	EC₅₀	2.2 μM Compound: 85; WZ4002	Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay	[PMID: 28603991]
A-431	EC₅₀	2.21 μM Compound: 7; WZ4002	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A549	GI₅₀	> 10 μM Compound: 5; WZ4002	Antiproliferative activity against human A549 cells harboring wild-type EGFR after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A549 cells harboring wild-type EGFR after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
A549	IC₅₀	1.87 μM Compound: 3; WZ4002	Antiproliferative activity against human A549 cells harboring wild type EGFR/k-Ras mutation after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR/k-Ras mutation after 72 hrs by MTT assay	[PMID: 26451770]
A549	IC₅₀	1.87 μM Compound: WZ4002	Antiproliferative activity against human A549 cells harboring wild type EGFR after 48 hrs by SRB assay Antiproliferative activity against human A549 cells harboring wild type EGFR after 48 hrs by SRB assay	[PMID: 28366268]
A549	IC₅₀	2.102 μM Compound: 1, WZ4002	Antiproliferative activity against k-RAS dependent human A549 cells overexpressing WT EGFR after 72 hrs by MTT assay Antiproliferative activity against k-RAS dependent human A549 cells overexpressing WT EGFR after 72 hrs by MTT assay	[PMID: 24607591]
A549	IC₅₀	2.102 μM Compound: 1, WZ4002	Cytotoxicity against human A549 cells harboring wild type EGFR and k-RAS mutation assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells harboring wild type EGFR and k-RAS mutation assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23668441]
A549	IC₅₀	3.354 μM Compound: WZ4002	Antiproliferative activity against wild type EGFR/k-Ras dependent human A549 cells after 72 hrs by MTT assay Antiproliferative activity against wild type EGFR/k-Ras dependent human A549 cells after 72 hrs by MTT assay	[PMID: 23792318]
A549	EC₅₀	3.99 μM Compound: 7; WZ4002	Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A549	IC₅₀	5.31 μM Compound: 1, WZ4002	Antiproliferative activity against human A549 cells expressing wild type EGFR coexpressing k-Ras mutant after 72 hrs by MTS assay Antiproliferative activity against human A549 cells expressing wild type EGFR coexpressing k-Ras mutant after 72 hrs by MTS assay	[PMID: 22339342]
BaF3	IC₅₀	> 1 μM Compound: 8, WZ4002	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay	[PMID: 26258521]
BaF3	EC₅₀	> 5000 nM Compound: WZ4002	Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	113 nM Compound: 3; WZ4002	Antiproliferative activity against mouse BA/F3 cells expressing wild type EGFR after 72 hrs by MTS assay Antiproliferative activity against mouse BA/F3 cells expressing wild type EGFR after 72 hrs by MTS assay	[PMID: 26882288]
BaF3	GI₅₀	2.2 μM Compound: 5; WZ4002	Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
BaF3	IC₅₀	2.82 μM Compound: 8, WZ4002	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by MTS assay Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by MTS assay	[PMID: 26258521]
BaF3	EC₅₀	26 nM Compound: WZ4002	Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	27 nM Compound: WZ4002	Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	3 nM Compound: 3; WZ4002	Antiproliferative activity against gefitinib sensitive mouse BA/F3 cells expressing EGFR exon 19 del E746_A750 activating mutant after 72 hrs by MTS assay Antiproliferative activity against gefitinib sensitive mouse BA/F3 cells expressing EGFR exon 19 del E746_A750 activating mutant after 72 hrs by MTS assay	[PMID: 26882288]
BaF3	GI₅₀	3.8 μM Compound: 3; WZ4002	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
BaF3	EC₅₀	31 nM Compound: WZ4002	Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	6258 nM Compound: WZ4002	Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	68 nM Compound: WZ4002	Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	8 nM Compound: 3; WZ4002	Antiproliferative activity against gefitinib resistant mouse BA/F3 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay Antiproliferative activity against gefitinib resistant mouse BA/F3 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay	[PMID: 26882288]
BaF3	IC₅₀	8 nM Compound: 8, WZ4002	Antiproliferative activity against mouse BA/F3 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay Antiproliferative activity against mouse BA/F3 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay	[PMID: 26258521]
BaF3	EC₅₀	989 nM Compound: WZ4002	Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BEAS-2B	IC₅₀	1.811 μM Compound: 1, WZ4002	Antiproliferative activity against human BEAS2B cells after 72 hrs by MTT assay Antiproliferative activity against human BEAS2B cells after 72 hrs by MTT assay	[PMID: 24607591]
BEAS-2B	IC₅₀	1.811 μM Compound: 1, WZ4002	Cytotoxicity against human BEAS2B cells harboring wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human BEAS2B cells harboring wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23668441]
CHO	GI₅₀	3.9 μM Compound: 5; WZ4002	Antiproliferative activity against CHO cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against CHO cells after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
HCC827	IC₅₀	0.007 μM Compound: 1, WZ4002	Antiproliferative activity against human HCC827 cells harboring EGFR del E746-A750 mutant after 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR del E746-A750 mutant after 72 hrs by MTS assay	[PMID: 22339342]
HCC827	GI₅₀	0.0074 μM Compound: 5; WZ4002	Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
HCC827	IC₅₀	0.008 μM Compound: 1, WZ4002	Antiproliferative activity against gefitinib-sensitive human HCC827 cells bearing EGFR del E746_A750 mutant after 72 hrs by MTT assay Antiproliferative activity against gefitinib-sensitive human HCC827 cells bearing EGFR del E746_A750 mutant after 72 hrs by MTT assay	[PMID: 24607591]
HCC827	IC₅₀	0.008 μM Compound: 1, WZ4002	Cytotoxicity against gefitinib-sensitive human HCC827 cells harboring EGFR E746_A740 deletion mutant assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against gefitinib-sensitive human HCC827 cells harboring EGFR E746_A740 deletion mutant assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23668441]
HCC827	IC₅₀	0.009 μM Compound: WZ4002	Antiproliferative activity against human HCC827 cells expressing EGFR E746_A750 deletion mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells expressing EGFR E746_A750 deletion mutant after 72 hrs by MTT assay	[PMID: 23792318]
HCC827	EC₅₀	0.02 μM Compound: 7; WZ4002	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
HCC827	IC₅₀	0.024 μM Compound: 1	Cytotoxicity against human HCC827 cells expressing EGFR kinase E746 to A750 deletion mutant after 72 hrs by MTS assay Cytotoxicity against human HCC827 cells expressing EGFR kinase E746 to A750 deletion mutant after 72 hrs by MTS assay	10.1039/C2MD20078C
HCC827	IC₅₀	12.4 nM Compound: WZ4002	Antiproliferative activity against gefitinib-sensitive human HCC827 cells harboring EGFR E746 to A750 deletion after 72 hrs by MTS assay Antiproliferative activity against gefitinib-sensitive human HCC827 cells harboring EGFR E746 to A750 deletion after 72 hrs by MTS assay	[PMID: 24053674]
HT-29	IC₅₀	2.95 μM Compound: 3; WZ4002	Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 26451770]
HT-29	IC₅₀	2.95 μM Compound: WZ4002	Antiproliferative activity against non-special gene type human HT-29 cells after 48 hrs by SRB assay Antiproliferative activity against non-special gene type human HT-29 cells after 48 hrs by SRB assay	[PMID: 28366268]
L02	IC₅₀	2.73 μM Compound: 1, WZ4002	Antiproliferative activity against human HL7702 cells expressing wilt type EGFR after 72 hrs by MTS assay Antiproliferative activity against human HL7702 cells expressing wilt type EGFR after 72 hrs by MTS assay	[PMID: 22339342]
L02	IC₅₀	9.15 μM Compound: 1	Cytotoxicity against human HL7702 cells expressing wild type EGFR after 72 hrs by MTS assay Cytotoxicity against human HL7702 cells expressing wild type EGFR after 72 hrs by MTS assay	10.1039/C2MD20078C
LoVo	IC₅₀	1.18 μM Compound: 6, WZ-4002	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: 23930994]
NCI-H1355	GI₅₀	5.3 μM Compound: 5; WZ4002	Antiproliferative activity against human NCI-H1355 cells harboring wild-type EGFR after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H1355 cells harboring wild-type EGFR after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
NCI-H1975	IC₅₀	0.023 μM Compound: 6, WZ-4002	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: 23930994]
NCI-H1975	IC₅₀	0.027 μM Compound: WZ-4002	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay	[PMID: 29534926]
NCI-H1975	IC₅₀	0.046 μM Compound: 1, WZ4002	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay	[PMID: 24607591]
NCI-H1975	IC₅₀	0.046 μM Compound: 1, WZ4002	Cytotoxicity against gefitinib-resistant human NCI-H1975 cells harboring EGFR L858R/T90M double mutant assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against gefitinib-resistant human NCI-H1975 cells harboring EGFR L858R/T90M double mutant assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23668441]
NCI-H1975	IC₅₀	0.048 μM Compound: 1, WZ4002	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTS assay	[PMID: 22339342]
NCI-H1975	IC₅₀	0.055 μM Compound: 3; WZ4002	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant by MTS assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant by MTS assay	[PMID: 26882288]
NCI-H1975	GI₅₀	0.056 μM Compound: 5; WZ4002	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
NCI-H1975	IC₅₀	0.058 μM Compound: 3; WZ4002	Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay	[PMID: 26451770]
NCI-H1975	IC₅₀	0.058 μM Compound: WZ4002	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 48 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 48 hrs by SRB assay	[PMID: 28366268]
NCI-H1975	IC₅₀	0.064 μM Compound: WZ4002	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by MTT assay	[PMID: 23792318]
NCI-H1975	IC₅₀	0.087 μM Compound: 1	Cytotoxicity against human NCI-H1975 cells expressing EGFR kinase L858R/T790M double mutant after 72 hrs by MTS assay Cytotoxicity against human NCI-H1975 cells expressing EGFR kinase L858R/T790M double mutant after 72 hrs by MTS assay	10.1039/C2MD20078C
NCI-H1975	EC₅₀	0.09 μM Compound: 7; WZ4002	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
NCI-H1975	IC₅₀	0.095 μM Compound: 1; WZ4002	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay	[PMID: 27131639]
NCI-H1975	EC₅₀	0.1 μM Compound: 85; WZ4002	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay	[PMID: 28603991]
NCI-H1975	IC₅₀	0.128 μM Compound: 1; WZ4002	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay	[PMID: 28987609]
NCI-H1975	IC₅₀	47 nM Compound: 12; WZ4002	Growth inhibition of human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay Growth inhibition of human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay	[PMID: 32432477]
NCI-H1975	IC₅₀	47 nM Compound: 3; WZ4002	Antiproliferative activity against gefitinib resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay Antiproliferative activity against gefitinib resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay	[PMID: 26882288]
NCI-H1975	IC₅₀	48.7 nM Compound: WZ4002	Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells expressing T790M/L858R mutation after 72 hrs by MTS assay Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells expressing T790M/L858R mutation after 72 hrs by MTS assay	[PMID: 24053674]
NCI-H2122	GI₅₀	5.7 μM Compound: 5; WZ4002	Antiproliferative activity against human NCI-H2122 cells harboring wild-type EGFR after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H2122 cells harboring wild-type EGFR after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
NCI-H3255	GI₅₀	0.39 μM Compound: 5; WZ4002	Antiproliferative activity against human H3255 cells harboring EGFR L858R mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human H3255 cells harboring EGFR L858R mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
PC-9	GI₅₀	0.027 μM Compound: 5; WZ4002	Antiproliferative activity against human PC9 cells harboring EGFR del19 mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human PC9 cells harboring EGFR del19 mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
PC-9	IC₅₀	0.044 μM Compound: 6, WZ-4002	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: 23930994]
PC-9	IC₅₀	14 nM Compound: 3; WZ4002	Antiproliferative activity against gefitinib resistant human PC9 cells expressing EGFR del E746_A750/T790M mutant after 72 hrs by MTS assay Antiproliferative activity against gefitinib resistant human PC9 cells expressing EGFR del E746_A750/T790M mutant after 72 hrs by MTS assay	[PMID: 26882288]
Sf9	IC₅₀	< 0.001 μM Compound: WZ4002	Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	< 0.001 μM Compound: WZ4002	Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	0.00019 μM Compound: WZ4002	Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) T790M/L858R mutant expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) T790M/L858R mutant expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay	[PMID: 25975640]
Sf9	IC₅₀	0.00042 μM Compound: WZ4002	Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) L858R mutant expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) L858R mutant expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay	[PMID: 25975640]
Sf9	IC₅₀	0.01 μM Compound: WZ4002	Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	0.016 μM Compound: WZ4002	Inhibition of wild type N-terminal His6-tagged human EGFR kinase domain (702 to 1016 residues) expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay Inhibition of wild type N-terminal His6-tagged human EGFR kinase domain (702 to 1016 residues) expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay	[PMID: 25975640]

体外研究
(In Vitro)

WZ4002 增加与抑制 NSCLC 细胞系中的 EGFR、AKT 和 ERK1/2 磷酸化以及表达不同 EGFR^T790M 突变等位基因的 NIH-3T3 细胞中的 EGFR 磷酸化相关的细胞效力。WZ4002 比 WT EGFR^[1] 更有效地抑制重组 L858R/T790M 蛋白的 EGFR 激酶活性^[1]。

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

体内研究
(In Vivo)

在药效学研究中，WZ4002 有效抑制 EGFR、AKT 和 ERK1/2 磷酸化，与单独使用载体处理的小鼠相比，这与 TUNEL 阳性细胞显著增加和 Ki67 阳性细胞显著减少有关。在为期 2 周的疗效研究中，与单独使用载体相比，WZ4002 处理在两种含有 T790M 的小鼠模型中均导致显著的肿瘤消退。处理后对肺部的组织学评估证实肿瘤结节明显消退，仅有少量小残留结节和结节残余物，这些证据表明处理效果具有细胞结构减少和纤维化增加，与重塑/瘢痕形成一致^[1] 。

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

分子量

494.97

Formula

C₂₅H₂₇ClN₆O₃

CAS 号

1213269-23-8

性状

固体

颜色

Light yellow 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 : 10 mg/mL (20.20 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	2.0203 mL	10.1016 mL	20.2032 mL
5 mM	0.4041 mL	2.0203 mL	4.0406 mL
10 mM	0.2020 mL	1.0102 mL	2.0203 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: 99.76%

选择批次：

Data Sheet (621 KB) SDS (393 KB)

COA (281 KB) LCMS (270 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.Nature. 2009 Dec 24;462(7276):1070-4. [Content Brief]

Kinase Assay ^[1]	EGFR kinase assay is performed using a GST-kinase fusion protein. The final reaction mixture contained 60 mM HEPES pH 7.5, 5 mM MgCl₂, 5 mM MnCl₂, 3 mM Na₃V0₄, 1.25 mM DTT, 20 μM ATP, 1.5 μM PTP1B (Tyr66) biotinylated peptide and 50 ng of EGFR kinase. A phospotyrosine mab (pTyr100) is used to detect phosphorylation of the EGFR substrate peptide in the presence of WZ4002, gefitinib or HKI-272 (concentration ranges 0-10 μM for all drugs) followed a fluorescent Anti-mouse IgG secondary antibody. Fluorescence emission is detected at 615 nm^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Growth and inhibition of growth is assessed by MTS assay. Ba/F3 cells are exposed to WZ4002 treatment for 72 hours. Growth and inhibition of growth is assessed by MTS assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Cohorts of EGFR TL/CCSP-rtTA and EGFR TD/CCSP-rtTA are put on doxycycline diet at 5 weeks of age to induce the expression of mutant EGFR. These mice undergo MRI after 6 to 8 weeks of doxycycline diet to document and quantify the lung cancer burden before being assigned to various treatment study cohorts. There is a minimum of 3 mice per treatment group. Mice are then treated either with vehicle (NMP 13 (10% 1-methyl-2-pyrrolidinone: 90% PEG-300) alone or WZ4002 at 25mg/kg gavage daily. After 2 weeks of treatment, these mice undergo a second round of MRI to document their response to the treatment. MRIs and tumor burden measurement are performed^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.Nature. 2009 Dec 24;462(7276):1070-4. [Content Brief]

WZ4002 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	2.0203 mL	10.1016 mL	20.2032 mL	50.5081 mL
	5 mM	0.4041 mL	2.0203 mL	4.0406 mL	10.1016 mL
	10 mM	0.2020 mL	1.0102 mL	2.0203 mL	5.0508 mL
	15 mM	0.1347 mL	0.6734 mL	1.3469 mL	3.3672 mL
	20 mM	0.1010 mL	0.5051 mL	1.0102 mL	2.5254 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:

WZ40021213269-23-8WZ 4002WZ-4002EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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：

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 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 © 2013-2024 MedChemExpress. All Rights Reserved.

WZ4002

Customer Review

MCE 顾客使用本产品发表的 8 篇科研文献

WZ4002 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

摩尔计算器

稀释计算器

WZ4002 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

WZ4002

Customer Review

WZ4002 相关抗体

MCE 顾客使用本产品发表的 8 篇科研文献

WZ4002 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

WZ4002 相关抗体:

摩尔计算器

稀释计算器

WZ4002 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z