WZ4002

Name: WZ4002
Brand: MedChemExpress
SKU: HY-12026
Rating: 5.0 (11 reviews)

Cat. No.: HY-12026 Purity: 99.76%: FAQs
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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.

For research use only. We do not sell to patients.

WZ4002 Chemical Structure

CAS No. : 1213269-23-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

8 Publications Citing Use of MCE WZ4002

: WZ4002 purchased from MedChemExpress. 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 MedChemExpress. 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 purchased from MedChemExpress. 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.

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Biological Activity
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Purity & Documentation
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Customer Review

Description

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)

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]

In Vitro

WZ4002 increases cellular potency correlated with inhibition of EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and EGFR phosphorylation in NIH-3T3 cells expressing different EGFR^T790M mutant alleles. WZ4002 inhibits EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR^[1].

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

In Vivo

In a pharmacodynamic study WZ4002 effectively inhibits EGFR, AKT and ERK1/2 phosphorylation which is associated with a significant increase in TUNEL positive and a significant decrease in Ki67 positive cells compared to vehicle alone treated mice. In a 2 week efficacy study, WZ4002 treatment results in significant tumor regressions compared to vehicle alone in both T790M containing murine models. Histological evaluation of the lungs following treatment confirms significant resolution of the tumor nodules with only few small residual nodules and nodule remnants that has evidence of treatment effect with decreased cellularity and increased fibrosis consistent with remodeling/scarring^[1].

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

Molecular Weight

494.97

Formula

C₂₅H₂₇ClN₆O₃

CAS No.

1213269-23-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

COC1=C(C=CC(N2CCN(CC2)C)=C1)NC3=NC=C(C(OC4=CC(NC(C=C)=O)=CC=C4)=N3)Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (20.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.76%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (244 KB) LCMS (270 KB)

Handling Instructions (2659 KB)

References

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

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

WZ4002 Related Classifications

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

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