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Submit ReviewZM 323881 hydrochloride
说明： Potent, selective inhibitor of VEGFR-2
化学名： 5-((7-Benzyloxyquinazolin-4-yl)amino)-4-fluoro-2-methylphenol hydrochloride
纯度： ≥99% (HPLC)
生物活性 for ZM 323881 hydrochloride
ZM 323881 hydrochloride is a potent and selective inhibitor of human vascular endothelial growth factor receptor 2 (VEGFR-2/KDR) activity. Selectively inhibits VEGFR-2 (IC50 = 2 nM) over VEGFR-1 and a range of other receptor tyrosine kinases such as PDGFRβ, FGFR1, EGFR and erbB2 (IC50 > 50 μM). Inhibits VEGF-A-induced endothelial cell proliferation in vitro (IC50 = 8 nM).
许可信息
Sold with the permission of AstraZeneca UK Ltd.
化合物库 for ZM 323881 hydrochloride
ZM 323881 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
技术数据 for ZM 323881 hydrochloride
| 分子量 | 411.86 |
| 公式 | C22H18FN3O2.HCl |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 193000-39-4 |
| PubChem ID | 22624897 |
| InChI Key | AVRHWGLIYGJSOD-UHFFFAOYSA-N |
| Smiles | Cl.CC1=C(O)C=C(NC2=C3C=CC(OCC4=CC=CC=C4)=CC3=NC=N2)C(F)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for ZM 323881 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 20.59 | 50 |
制备储备液 for ZM 323881 hydrochloride
以下数据基于产品分子量 411.86。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.86 mL | 24.28 mL | 48.56 mL |
| 2.5 mM | 0.97 mL | 4.86 mL | 9.71 mL |
| 5 mM | 0.49 mL | 2.43 mL | 4.86 mL |
| 25 mM | 0.1 mL | 0.49 mL | 0.97 mL |
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产品说明书 for ZM 323881 hydrochloride
参考文献 for ZM 323881 hydrochloride
参考文献是支持产品生物活性的出版物。
Whittles et al (2002) ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity. Microcirculation 9 513 PMID: 12483548
Endo et al (2003) Selective inhibition of vascular endothelial growth factor receptor-2 (VEGFR-2) identifies a central role for VEGFR-2 in human aortic endothelial cell responses to VEGF. J.Recept.Signal Transduct.Res. 23 239 PMID: 14626450
If you know of a relevant reference for ZM 323881 hydrochloride, please let us know.
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关键词: ZM 323881 hydrochloride, ZM 323881 hydrochloride supplier, Potent, selective, inhibitors, inhibits, VEGFR-2, Vascular, Endothelial, Growth, Factor, Receptors, KDR, Flt, Receptor, Tyrosine, Kinases, RTKs, ZM323881, hydrochloride, AstraZeneca, VEGFR, 2475, Tocris Bioscience
11 篇 ZM 323881 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 ZM 323881 hydrochloride 的部分引用包括：
Holmes et al (2010) VEGF stimulates RCAN1.4 expression in endothelial cells via a pathway requiring Ca2+/calcineurin and protein kinase C-delta. PLoS One 5 e11435 PMID: 20625401
Chandrasekharan et al (2010) Synergistic induction of mitogen-activated protein kinase phosphatase-1 by thrombin and epidermal growth factor requires vascular endothelial growth factor receptor-2. Biomed Rep 30 1983 PMID: 20671228
Busceti et al (2018) Dickkopf-3 Causes Neuroprotection by Inducing Vascular Endothelial Growth Factor. Front Cell Neurosci 12 292 PMID: 30258353
Durré et al (2018) uPARAP/Endo180 receptor is a gatekeeper of VEGFR-2/VEGFR-3 heterodimerisation during pathological lymphangiogenesis. Nat Commun 9 5178 PMID: 30518756
Kawakami et al (2011) Investigation of a novel molecular descriptor for the lead optimization of 4-aminoquinazolines as vascular endothelial growth factor receptor-2 inhibitors: application for quantitative structure-activity relationship analysis in lead optimization. PLoS One 21 1371 PMID: 21306896
Maertens et al (2014) Bone marrow-derived mesenchymal stem cells drive lymphangiogenesis. Arterioscler Thromb Vasc Biol 9 e106976 PMID: 25222747
Zhong et al (2011) Combinatory action of VEGFR2 and MAP kinase pathways maintains endothelial-cell integrity. Cell Res 21 1080 PMID: 21423276
Lakshmikanthan et al (2011) Rap1 promotes VEGFR2 activation and angiogenesis by a mechanism involving integrin αvβ?. Blood 118 2015 PMID: 21636859
Page et al (2019) Positive Feedback Defines the Timing, Magnitude, and Robustness of Angiogenesis. Cell Rep 27 3139 PMID: 31189101
Hulse et al (2016) The control of alternative splicing by SRSF1 in myelinated afferents contributes to the development of neuropathic pain. Neurobiol Dis 96 186 PMID: 27616424
Huang et al (2010) Pharmacological and genetic accumulation of hypoxia-inducible factor-1alpha enhances excitatory synaptic transmission in hippocampal neurons through the production of vascular endothelial growth factor. J Neurosci 30 6080 PMID: 20427666
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
Pathways for ZM 323881 hydrochloride
