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Technical Data
| Formula | C22H18FN3O2.HCl |
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| Molecular Weight | 411.86 | CAS No. | 193000-39-4 | |
| Solubility (25°C)* | In vitro | DMSO | 10 mg/mL (24.28 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2. | ||
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| 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. [1] 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. [2] 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. [3] 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. [4] 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. [5] |
Protocol (from reference)
References
Customer Product Validation
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Data from [Data independently produced by , , Biochem Pharmacol, 2017, 132:29-37]
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Data from [Data independently produced by , , Biochem Pharmacol, 2017, 132:29-37]
Selleck's ZM 323881 HCl has been cited by 20 publications
| The Antioxidant TEMPOL Protects Human Hematopoietic Stem Cells From Culture-Mediated Loss of Functions [ Stem Cells Transl Med, 2023, szad049] | PubMed: 37616262 |
| The Antioxidant TEMPOL Protects Human Hematopoietic Stem Cells From Culture-Mediated Loss of Functions [ Stem Cells Transl Med, 2023, 12(10):676-688] | PubMed: 37616262 |
| Phosphate-induced activation of VEGFR2 leads to caspase-9-mediated apoptosis of hypertrophic chondrocytes [ iScience, 2023, 26(9):107548] | PubMed: 37636062 |
| Phosphate-induced activation of VEGFR2 leads to caspase-9-mediated apoptosis of hypertrophic chondrocytes [ iScience, 2023, 26(9):107548] | PubMed: 37636062 |
| Phosphate-induced activation of VEGFR2 leads to caspase-9-mediated apoptosis of hypertrophic chondrocytes [ iScience, 2023, 26(9):107548] | PubMed: 37636062 |
| Histamine promotes angiogenesis through a histamine H1 receptor-PKC-VEGF-mediated pathway in human endothelial cells [ J Pharmacol Sci, 2023, 151(4):177-186] | PubMed: 36925216 |
| Bone marrow-independent adventitial macrophage progenitor cells contribute to angiogenesis [ Cell Death Dis, 2022, 13(3):220] | PubMed: 35264563 |
| Intrinsic epigenetic control of angiogenesis in induced pluripotent stem cell-derived endothelium regulates vascular regeneration [ NPJ Regen Med, 2022, 7(1):28] | PubMed: 35551465 |
| Vascular endothelial growth factor-A/vascular endothelial growth factor2 signaling in spinal neurons contributes to bone cancer pain [ Mol Pain, 2022, 18:17448069221075891] | PubMed: 35083936 |
| Low-flow intussusception and metastable VEGFR2 signaling launch angiogenesis in ischemic muscle [ Sci Adv, 2021, 7(48):eabg9509] | PubMed: 34826235 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.