ZM 323881 HCl

製品コードS2896 バッチS289601

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₂H₁₈FN₃O₂.HCl

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	ZM 323881は、強力で選択的なVEGFR2阻害剤であり、IC50は2 nM未満で、VEGFR1、PDGFRβ、FGFR1、EGFR、およびErbB2にはほとんど活性がありません。
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.

製品説明

ZM 323881は、強力で選択的なVEGFR2阻害剤であり、IC50は2 nM未満で、VEGFR1、PDGFRβ、FGFR1、EGFR、およびErbB2にはほとんど活性がありません。

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.

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assay
キナーゼアッセイ	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.

参考

https://pubmed.ncbi.nlm.nih.gov/12483548/
https://pubmed.ncbi.nlm.nih.gov/14626450/
https://pubmed.ncbi.nlm.nih.gov/16499871/

https://pubmed.ncbi.nlm.nih.gov/17686471/
https://pubmed.ncbi.nlm.nih.gov/17211450/

+ 展开

カスタマーフィードバック

: Data from [Data independently produced by , , Biochem Pharmacol, 2017, 132:29-37]

: Data from [Data independently produced by , , Biochem Pharmacol, 2017, 132:29-37]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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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
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
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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
Contribution of Adventitia-Derived Stem and Progenitor Cells to New Vessel Formation in Tumors [ Cells, 2021, 10(7)1719]	PubMed: 34359889

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。

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