CAS 193000-39-4|ZM 323881 HCl

Introduction：Basic information about CAS 193000-39-4|ZM 323881 HCl, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. ZM 323881 HCl BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	ZM 323881 HCl
CAS Number	193000-39-4	Molecular Weight	411.857
Density	/	Boiling Point	/
Molecular Formula	C₂₂H₁₉ClFN₃O₂	Melting Point	/
MSDS	/	Flash Point	/

Names

Name	5-{[7-(Benzyloxy)-4-quinazolinyl]amino}-4-fluoro-2-methylphenol h ydrochloride (1:1)
Synonym	More Synonyms

ZM 323881 HCl BiologicalActivity

Description	ZM323881 hydrochloride is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
Related Catalog	Research Areas >>Cancer
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.

Chemical & Physical Properties

Molecular Formula	C₂₂H₁₉ClFN₃O₂
Molecular Weight	411.857
Exact Mass	411.114990
PSA	67.27000
LogP	5.98050
InChIKey	AVRHWGLIYGJSOD-UHFFFAOYSA-N
SMILES	Cc1cc(F)c(Nc2ncnc3cc(OCc4ccccc4)ccc23)cc1O.Cl
Storage condition	-20℃

Synonyms

ZM 323881 HCl

5-{[7-(Benzyloxy)quinazolin-4-yl]amino}-4-fluoro-2-methylphenol hydrochloride (1:1)

Phenol, 4-fluoro-2-methyl-5-[[7-(phenylmethoxy)-4-quinazolinyl]amino]-, hydrochloride (1:1)

5-{[7-(Benzyloxy)-4-quinazolinyl]amino}-4-fluoro-2-methylphenol hydrochloride (1:1)

ZM 323881 hydrochloride

5-[(7-Benzyloxyquinazolin-4-yl)amino]-4-fluoro-2-methylphenol hydrochloride

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