Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Purity: ≥98%
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.
Targets |
VEGFR2 (IC50 = 2 nM)
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ln Vitro |
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ln Vivo |
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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].
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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].
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Animal Protocol |
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References |
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Molecular Formula |
C22H18FN3O2.HCL
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Molecular Weight |
411.85656
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Exact Mass |
375.14
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Elemental Analysis |
C, 64.16; H, 4.65; Cl, 8.61; F, 4.61; N, 10.20; O, 7.77
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CAS # |
193000-39-4
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Appearance |
Solid powder
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SMILES |
CC1=CC(=C(C=C1O)NC2=NC=NC3=C2C=CC(=C3)OCC4=CC=CC=C4)F.Cl
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InChi Key |
AVRHWGLIYGJSOD-UHFFFAOYSA-N
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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
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Chemical Name |
4-fluoro-2-methyl-5-[(7-phenylmethoxyquinazolin-4-yl)amino]phenol;hydrochloride
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Synonyms |
ZM323881; ZM 323881; ZM323881 hydrochloride; ZM-323881; ZM323881 HCl; ZM 323881 hydrochloride; ZM-323881 hydrochloride; ZM 323881 HCl; ZM-323881 HCl
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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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.
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.
(2) Be sure to add the solvent(s) in order.