ZM 323881 HCl

Alias: ZM323881; ZM 323881; ZM323881 hydrochloride; ZM-323881; ZM323881 HCl; ZM 323881 hydrochloride; ZM-323881 hydrochloride; ZM 323881 HCl; ZM-323881 HCl
Cat No.:V0523 Purity: ≥98%
ZM323881 HCl (ZM-323881 Hydrochloride) is a novel, potent and selective tyrosine kinase VEGFR2 inhibitor with potential antitumor activity.
ZM 323881 HCl Chemical Structure CAS No.: 193000-39-4
Product category: VEGFR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
Other Sizes

Other Forms of ZM 323881 HCl:

  • ZM323881
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

ZM323881 HCl (ZM-323881 Hydrochloride) is a novel, potent and selective tyrosine kinase VEGFR2 inhibitor with potential antitumor activity. It exhibits little to no activity against other kinases like PDGFRβ, FGFR1, ErbB2, VEGFR1, and FGFR1. It inhibits human vascular endothelial growth factor receptor 2 (VEGFR2) with an IC50 of less than 2 nM. ZM-323881. ZM323881 suppresses VEGF-R2 tyrosine phosphorylation and VEGF-A-induced endothelial cell proliferation in vitro (IC50 = 8 nM). At 30 minutes, ZM323881 (10 nM) inhibits Rac1 activation induced by VEGF in HUVECs.

Biological Activity I Assay Protocols (From Reference)
Targets
VEGFR2 (IC50 = 2 nM)
ln Vitro

ZM323881 is an anilinoquinazoline that exhibits excellent selectivity against PDGFRβ, FGFR1, EGFR, and erbB2 (IC50>50 μM) and potently inhibits VEGFR2 (KDR) tyrosine kinase activity. ZM323881 suppresses VEGFR2 tyrosine phosphorylation and VEGF-A-induced endothelial cell proliferation (IC50=8 nM)[1]. ZM323881 blocks VEGFR-2 activation, but not VEGFR-1, platelet-derived growth factor receptor (PDGFR), hepatocyte growth factor (HGF) receptor, or epidermal growth factor receptor (EGFR). ZM323881, at 1 μM, totally prevents VEGF-induced ERK phosphorylation in HAECs[2].

ln Vivo

Enzyme Assay
Compounds (ZM323881) are incubated (20 minutes at room temperature) with the enzyme in 96-well plates coated with a poly(Glu, Ala, Tyr) 6:3:1 random copolymer substrate, in an N-2-hydroxyethylpiperazine-N'-2-ethanesulphonate (HEPES) (pH 7.5) buffered solution with 10 mM MnCl2 and 2 μM ATP. The next step involves the sequential incubation of sheep anti-mouse Ig antibody linked to horseradish peroxidase (HRP), mouse IgG anti-phosphotyrosine antibody, and 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) in order to detect phosphorylated tyrosine. Nonlin-ear regression is utilized to interpolate IC50 data [1].
Cell Assay
Plated at passages 2–8, HUVEC cells isolated from umbilical cords are dosed with ZM323881±VEGF-A (3 ng/mL), EGF (3 ng/mL), or basic fibroblast growth factor (bFGF, 0.3 ng/mL) in 96-wellplates (1000 cells/well). After that, the cultures are incubated for four days. Day 4: The cultures are re-incubated for 4 hours after being pulsed with 1 μCi/well of 3H-thymidine. After that, the cells are taken out and tested with a beta-counter to see if tritium has been incorporated. Interpolated IC50 data are used[1].
Animal Protocol


References

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

[2]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H18FN3O2.HCL
Molecular Weight
411.85656
Exact Mass
375.14
Elemental Analysis
C, 64.16; H, 4.65; Cl, 8.61; F, 4.61; N, 10.20; O, 7.77
CAS #
193000-39-4
Appearance
Solid powder
SMILES
CC1=CC(=C(C=C1O)NC2=NC=NC3=C2C=CC(=C3)OCC4=CC=CC=C4)F.Cl
InChi Key
AVRHWGLIYGJSOD-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H18FN3O2.ClH/c1-14-9-18(23)20(11-21(14)27)26-22-17-8-7-16(10-19(17)24-13-25-22)28-12-15-5-3-2-4-6-15;/h2-11,13,27H,12H2,1H3,(H,24,25,26);1H
Chemical Name
4-fluoro-2-methyl-5-[(7-phenylmethoxyquinazolin-4-yl)amino]phenol;hydrochloride
Synonyms
ZM323881; ZM 323881; ZM323881 hydrochloride; ZM-323881; ZM323881 HCl; ZM 323881 hydrochloride; ZM-323881 hydrochloride; ZM 323881 HCl; ZM-323881 HCl
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~10 mg/mL (~24.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
1% CMC Na: 20 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4280 mL 12.1400 mL 24.2801 mL
5 mM 0.4856 mL 2.4280 mL 4.8560 mL
10 mM 0.2428 mL 1.2140 mL 2.4280 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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