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ZM 323881 HCl VEGFR inhibitor

Cat.No.S2896

ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2.
ZM 323881 HCl VEGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 411.86

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Quality Control

Batch: S289601 DMSO]10 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.90%
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99.90

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (24.28 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 411.86 Formula

C22H18FN3O2.HCl

 Storage (From the date of receipt)
CAS No. 193000-39-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC(=C(C=C1O)NC2=NC=NC3=C2C=CC(=C3)OCC4=CC=CC=C4)F.Cl

Mechanism of Action

Targets/IC50/Ki
VEGFR2
<2 nM
In vitro
ZM323881 inhibits VEGF-A, EGF and bFEF induced HUVEC cell proliferation with IC50 of 8 nM, 1.9 μM and 1.6 μM, respectively. ZM323881 (10 nM) abolishes VEGF-A-mediated increases in vascular permeability in perfused mesenteric microvessels in male leopard. ZM323881 (10 nM) blocks the increase in intensity of the VEGF-R2 band in the lung of male leopard frogs. ZM323881 (1 μM) blocks activation of extracellular regulated-kinase, p38, Akt, and endothelial nitric oxide synthetase (eNOS) by VEGF, but did not inhibit p38 activation by the VEGFR-1-specific ligand, placental growth factor (PIGF) in human aortic endothelial cells (HAECs). ZM323881 (1 μM) also perturbes VEGF-induced membrane extension, cell migration, and tube formation by HAECs. ZM323881 (1 μM) reverses VEGF-stimulated phosphorylation of CrkII and its Src homology 2 (SH2)-binding protein p130Cas, which are known to play a pivotal role in regulating endothelial cell migration. ZM323881 (10 nM) completely blocks VEGF-induced VEGF promoter activity in SCC-9 cells. ZM323881 (10 nM) blocks VEGF stimulated Hif-1α protein accumulation in SCC-9 cells. ZM323881 (10 nM) blocks VEGF-induced Rac1 activation at 30 min in HUVECs. ZM323881 (10 nM) prevents Vav2 tyrosine phosphorylation in response to VEGF in HUVECs. ZM323881 (< 1 μM) inhibits VEGF stimulated neural stem cell proliferation in a dose-dependent manner. ZM323881 (< 1 μM) inhibits neural stem cell proliferation in a dose-dependent manner even when no exogenous VEGF is added.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/17686471/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17211450/

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