ZM323881

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ZM323881 is a potent and selective VEGFR2 inhibitor with an IC₅₀ of less than 2 nM.

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

ZM323881 Chemical Structure

CAS No. : 193001-14-8

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Other In-stock Forms of ZM323881:

ZM323881 hydrochloride

Other Forms of ZM323881:

ZM323881 hydrochloride In-stock

2 Publications Citing Use of MCE ZM323881

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•Related Small Molecules:

•Related Proteins:

View All VEGFR Isoform Specific Products:

View All Isoforms

VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

Biological Activity
Protocol
Purity & Documentation
References
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Description

ZM323881 is a potent and selective VEGFR2 inhibitor with an IC₅₀ of less than 2 nM.

IC₅₀ & Target^[1]

VEGFR2

2 nM (IC₅₀)

In Vitro

ZM323881 is an anilinoquinazoline that potently inhibits VEGFR2 (KDR) tyrosine kinase activity anddemonstrates excellent selectivity versus other receptor tyrosine kinases, including PDGFRβ, FGFR1, EGFR and erbB2 (IC₅₀>50 μM). ZM323881 inhibits VEGF-A-induced endothelial cell proliferation(IC₅₀=8 nM) and VEGFR2 tyrosine phosphorylation^[1]. ZM323881 inhibits activation of VEGFR-2, but not of VEGFR-1, epidermal growth factor receptor (EGFR), platelet-derived growth factor receptor (PDGFR), or hepatocyte growth factor (HGF) receptor. In HAECs, ZM323881 completely inhibits VEGF-induced ERK phosphorylation at 1 μM^[2].

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

Molecular Weight

375.40

Formula

C₂₂H₁₈FN₃O₂

CAS No.

193001-14-8

SMILES

CC1=C(O)C=C(NC2=C3C=CC(OCC4=CC=CC=C4)=CC3=NC=N2)C(F)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Whittles CE, et al. ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity. Microcirculation. 2002 Dec;9(6):513-22. [Content Brief]

[2]. Endo A, et al. Selective inhibition of vascular endothelial growth factor receptor-2 (VEGFR-2) identifies a central role for VEGFR-2 in human aortic endothelial cell responses to VEGF. J Recept Signal Transduct Res. 2003;23(2-3):239-54. [Content Brief]

Kinase Assay ^[1]	Compounds (ZM323881) are incubated (20 minutes, room temperature) with enzyme in an N-2-hydroxyethylpiperazine-N'-2-ethanesulphonate (HEPES) (pH 7.5) buffered solution containing 10 mM MnCl₂ and 2 μM ATP, in96-well plates coated with a poly(Glu, Ala, Tyr) 6:3:1 random copolymer substrate. Phosphorylated tyrosine is then detected bysequential incubation with mouse IgG anti-phosphotyrosine antibody a horseradish peroxidase(HRP)-linked sheep anti-mouse Ig antibody and 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid). IC₅₀ data are interpolated by nonlin-ear regression^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	HUVEC cells isolated from umbilical cords are plated (at passage 2–8) in 96-wellplates (1000 cells/well) and dosed with ZM323881±VEGF-A (3 ng/mL), EGF (3 ng/mL), or basicfibroblast growth factor (bFGF, 0.3 ng/mL). The cultures are then incubated for 4 days. On day 4, the cultures are pulsed with 1 μCi/well of ³H-thymidine and reincubated for 4 hours. The cells are then harvested and assayed for the incorporation of tritium by using a beta-counter. IC₅₀ data are interpolated^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Whittles CE, et al. ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity. Microcirculation. 2002 Dec;9(6):513-22. [Content Brief] [2]. Endo A, et al. Selective inhibition of vascular endothelial growth factor receptor-2 (VEGFR-2) identifies a central role for VEGFR-2 in human aortic endothelial cell responses to VEGF. J Recept Signal Transduct Res. 2003;23(2-3):239-54. [Content Brief]

ZM323881 Related Classifications

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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:

ZM323881193001-14-8ZM 323881ZM-323881VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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