受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H18FN3O2.HCl |
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分子量 | 411.86 | CAS No. | 193000-39-4 | |
Solubility (25°C)* | 体外 | DMSO | 10 mg/mL (24.28 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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. |
製品説明 | 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] |
キナーゼアッセイ | Binding assay | |
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ZM323881 is incubated (20 minutes, room temperature) with enzyme in an HEPES (pH 7.5) buffered solution containing 10 mM MnCl2 and 2 μM ATP, in 96-well plates coated with a poly(Glu, Ala, Tyr) 6:3:1 random copolymer substrate. IC50 data are interpolated by nonlinear regression (four-parameter logistic equation) using Microcal Origin software. |
Data from [Data independently produced by , , Biochem Pharmacol, 2017, 132:29-37]
Data from [Data independently produced by , , Biochem Pharmacol, 2017, 132:29-37]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。