1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. ZM323881

ZM323881 

Cat. No.: HY-15467
Handling Instructions

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

ZM323881 Chemical Structure

CAS No. : 193001-14-8

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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].

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.

References
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
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ZM323881
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