ZM323881VEGFR-2/KDR inhibitor,potent and selective CAS# 193001-14-8 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 193001-14-8 | SDF | Download SDF |
PubChem ID | 16759369 | Appearance | Powder |
Formula | C22H18FN3O2 | M.Wt | 375.4 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO | ||
Chemical Name | 4-fluoro-2-methyl-5-[(7-phenylmethoxyquinazolin-4-yl)amino]phenol | ||
SMILES | CC1=CC(=C(C=C1O)NC2=NC=NC3=C2C=CC(=C3)OCC4=CC=CC=C4)F | ||
Standard InChIKey | NVBNDZZLJRYRPD-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C22H18FN3O2/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) | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | ZM323881 is a potent and selective inhibitor of human vascular endothelial growth factor receptor 2 (VEGFR-2/KDR) with IC50 value of 2 nM. | |||||
Targets | VEGFR-2/KDR | |||||
IC50 | 2 nM |
ZM323881 Dilution Calculator
ZM323881 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.6638 mL | 13.3191 mL | 26.6383 mL | 53.2765 mL | 66.5956 mL |
5 mM | 0.5328 mL | 2.6638 mL | 5.3277 mL | 10.6553 mL | 13.3191 mL |
10 mM | 0.2664 mL | 1.3319 mL | 2.6638 mL | 5.3277 mL | 6.6596 mL |
50 mM | 0.0533 mL | 0.2664 mL | 0.5328 mL | 1.0655 mL | 1.3319 mL |
100 mM | 0.0266 mL | 0.1332 mL | 0.2664 mL | 0.5328 mL | 0.666 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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ZM323881 inhibits VEGF-A-induced endothelial cell proliferation (IC50 = 8 nM) and VEGF-R2 tyrosine phosphorylation (IC50 < 2 nM).
Vascular endothelial growth factor (VEGF) increases vascular permeability and angiogenesis in many pathological conditions, such as cancer, arthritis, and diabetes. VEGF activates VEGF-Receptor 1 (VEGF-R1) and VEGF-Receptor 2 (VEGF-R2) that autophosphorylate to initiate a signaling cascade resulting in angiogenesis and increased microvascular permeability. ZM323881 is a potent and selective inhibitor of VEGF-R2 tyrosine kinase.
In vitro: ZM323881 was found to inhibit VEGF-A-induced endothelial cell proliferation (IC50 = 8 nM) and VEGF-R2 tyrosine phosphorylation in vitro (IC50 < 2 nM) [1].
In vivo: VEGF-Amediated increases in vascular permeability in perfused mesenteric microvessels in vivo were reversibly abolished by both ZM323881 and the class III receptor tyrosine kinase inhibitor PTK787/ZK222584, suggesting that VEGF-R2 phosphorylation is necessary for VEGF-A-mediated increases in microvascular permeability in vivo [1].
Clinical trials: There is no clinical data are available currenlty.
Reference:
[1] Whittles CE, Pocock TM, Wedge SR, Kendrew J, Hennequin LF, Harper SJ, Bates DO. ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity. Microcirculation. 2002;9(6):513-22.
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ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity.[Pubmed:12483548]
Microcirculation. 2002 Dec;9(6):513-22.
OBJECTIVE: Vascular endothelial growth factor (VEGF) increases vascular permeability and angiogenesis in many pathological conditions including cancer, arthritis, and diabetes. VEGF activates VEGF-Receptor 1(VEGF-R1) and VEGF-Receptor 2 (VEGF-R2), which autophosphorylate to initiate a signaling cascade resulting in angiogenesis and increased microvascular permeability. Here we describe a novel VEGF-R2 selective inhibitor, ZM323881 (5-[[7-(benzyloxy) quinazolin-4-yl]amino]-4-fluoro-2-methylphenol), that is a potent and selective inhibitor of VEGF-R2 tyrosine kinase in vitro (IC(50) < 2 nM), compared with other receptor tyrosine kinases, including VEGF-R1 (IC(50) > 50 microM). METHODS: Endothelial cell proliferation was assayed by (3)H-thymidine incorporation in response to VEGF-A +/- ZM323881. The effect of ZM323881 on VEGF-mediated permeability was measured in frog microvessels using the Landis Michel technique. To ensure that ZM323881 was effective in frogs, western analysis was performed on protein extracted from frog lungs incubated in the presence or absence of VEGF-A or VEGF-A with ZM323881. RESULTS: ZM323881 inhibits VEGF-A-induced endothelial cell proliferation (IC(50) = 8 nM) and VEGF-R2 tyrosine phosphorylation in vitro. VEGF-A-mediated increases in vascular permeability in perfused mesenteric microvessels in vivo were reversibly abolished by both ZM323881 and the class III receptor tyrosine kinase inhibitor PTK787/ZK222584. CONCLUSIONS: These data suggest that VEGF-R2 phosphorylation is necessary for VEGF-A-mediated increases in microvascular permeability in vivo.
Selective reversal of BCRP-mediated MDR by VEGFR-2 inhibitor ZM323881.[Pubmed:28242251]
Biochem Pharmacol. 2017 May 15;132:29-37.
The expression of breast cancer resistant protein (BCRP) in lung cancer is correlated with development of multidrug resistance (MDR) and therefore leads to lower response to chemotherapy. ZM323881, a previously developed selective VEGFR-2 inhibitor, was found to have inhibitory effects on BCRP-mediated MDR in this investigation. ZM323881 significantly decreased the cytotoxic doses of mitoxantrone and SN-38 in BCRP-overexpressing NCI-H460/MX20 cells. Mechanistic studies revealed that ZM323881 effected by inhibiting BCRP-mediated drug efflux, leading to intracellular accumulation of BCRP substrates. No significant alteration in the expression levels and localization pattern of BCRP was observed when BCRP-overexpressing cells were exposed to ZM323881. Stimulated bell-shaped ATPase activities were observed. Molecular docking suggested that ZM323881 binds to the modulator site of BCRP and the binding pose is stable validated by 100ns molecular dynamic simulation. Overall, our results indicated that ZM323881 reversed BCRP-related MDR by inhibiting its efflux function. These findings might be useful in developing combination chemotherapy for MDR cancer treatment.