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193001-14-8

193001-14-8 structure
193001-14-8 structure
  • Name: ZM323881
  • Chemical Name: 4-fluoro-2-methyl-5-[(7-phenylmethoxyquinazolin-4-yl)amino]phenol
  • CAS Number: 193001-14-8
  • Molecular Formula: C22H18FN3O2
  • Molecular Weight: 375.39600
  • Catalog: Research Areas Cancer
  • Create Date: 2016-02-02 00:29:52
  • Modify Date: 2024-01-02 16:14:25
  • ZM323881 is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
Name 4-fluoro-2-methyl-5-[(7-phenylmethoxyquinazolin-4-yl)amino]phenol
Synonyms cs-0986
ZM323881
Description ZM323881 is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
Related Catalog
Target

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].
Kinase Assay 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].
Cell Assay 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].
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.

[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.
Molecular Formula C22H18FN3O2
Molecular Weight 375.39600
Exact Mass 375.13800
PSA 67.27000
LogP 5.17850
Storage condition 2-8℃

Chemsrc provides CAS#:193001-14-8 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 193001-14-8 | Chemsrc address: https://m.chemsrc.com/en/baike/617251.html

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