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Submit ReviewZM 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).
Sold with the permission of AstraZeneca UK Ltd.
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。
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 20.59 | 50 |
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 |
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.
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
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:
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
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
Lakshmikanthan et al (2011) Rap1 promotes VEGFR2 activation and angiogenesis by a mechanism involving integrin αvβ?. Blood 118 2015 PMID: 21636859
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
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
Page et al (2019) Positive Feedback Defines the Timing, Magnitude, and Robustness of Angiogenesis. Cell Rep 27 3139 PMID: 31189101
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
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
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
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