193001-14-8
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
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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 |
| Molecular Formula | C22H18FN3O2 |
|---|---|
| Molecular Weight | 375.39600 |
| Exact Mass | 375.13800 |
| PSA | 67.27000 |
| LogP | 5.17850 |
| Storage condition | 2-8℃ |