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Submit ReviewAG 490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Inhibitor of JAK2, JAK3/STAT, JAK3/AP-1 and JAK3/MAPK pathways and potently inhibits cytokine-independent cell growth in vitro and tumor cell invasion in vivo.
分子量 | 294.31 |
公式 | C17H14N2O3 |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 133550-30-8 |
PubChem ID | 5328779 |
InChI Key | TUCIOBMMDDOEMM-RIYZIHGNSA-N |
Smiles | OC1=C(O)C=C(\C=C(/C#N)C(=O)NCC2=CC=CC=C2)C=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 | |||
ethanol | 5.89 | 20 | |
DMSO | 29.43 | 100 |
以下数据基于产品分子量 294.31。 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 |
---|---|---|---|
1 mM | 3.4 mL | 16.99 mL | 33.98 mL |
5 mM | 0.68 mL | 3.4 mL | 6.8 mL |
10 mM | 0.34 mL | 1.7 mL | 3.4 mL |
50 mM | 0.07 mL | 0.34 mL | 0.68 mL |
参考文献是支持产品生物活性的出版物。
Abe et al (2009) The polycythemia vera-associated Jak2 V617F mutant induces tumorigenesis in nude mice. Int.Immunopharmacol. 9 870 PMID: 19327411
Gazit et al (1991) Tyrphostins. 2. Heterocyclic and α-substituted benzylidenemalononitrile tyrophostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J.Med.Chem. 34 1896 PMID: 1676428
Meydan et al (1996) Inhbition of acute lymphoblastic leukaemia by a JAK-2 inhibitor. Nature 379 645 PMID: 8628398
Wang et al (1999) JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response. J.Immunol. 162 3897 PMID: 10201908
If you know of a relevant reference for AG 490, please let us know.
关键词: AG 490, AG 490 supplier, JAK2, JAK3, inhibitors, inhibits, EGFR-kinase, JAK, Kinase, Cytokine, NF-κB, NF-kappaB, Signaling, Signalling, Janus, Activated, Kinases, Epidermal, Growth, Factors, Receptors, ErbB, Her, EGFR, RTK, Receptor, Tyrosine, RTKs, AG490, Tyrphostin, AG, 490, 0414, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AG 490 的部分引用包括:
Kubota et al (2014) mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways. PLoS One 9 e106316 PMID: 25181481
Rogers and Gahring (2015) Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways. EMBO J 10 e0143319 PMID: 26619345
Doulatov et al (2009) PLZF is a regulator of homeostatic and cytokine-induced myeloid development. Genes Dev 23 2076 PMID: 19723763
Azad et al (2017) PD-L1 blockade enhances response of pancreatic ductal adenocarcinoma to radiotherapy. EMBO Mol Med 9 167 PMID: 27932443
Fontaine et al (2008) IL-9/IL-9 receptor signaling selectively protects cortical neurons against developmental apoptosis. Cell Death Differ 15 1542 PMID: 18551134
Lu et al (2008) JAK/STAT and PI3K/AKT pathways form a mutual transactivation loop and afford resistance to oxidative stress-induced apoptosis in cardiomyocytes. Cell Physiol Biochem 21 305 PMID: 18441519
Zhao et al (2015) Evodiamine Induces Apoptosis and Inhibits Migration of HCT-116 Human Colorectal Cancer Cells. J Transl Med 16 27411 PMID: 26580615
Jiang et al (2015) YangZheng XiaoJi exerts anti-tumour growth effects by antagonising the effects of HGF and its receptor, cMET, in human lung cancer cells. PLoS One 13 280 PMID: 26310485
Shenoy et al (2015) Let-7 and miR-125 cooperate to prime progenitors for astrogliogenesis. Neuropsychopharmacology 34 1180 PMID: 25715649
Tactacan et al (2015) The pseudokinase SgK223 promotes invasion of pancreatic ductal epithelial cells through JAK1/Stat3 signaling. Mol Cancer 14 139 PMID: 26215634
Park et al (2013) Inactivation of JAK2/STAT3 signaling axis and downregulation of M1 mAChR cause cognitive impairment in klotho mutant mice, a genetic model of aging. Neuron 38 1426 PMID: 23389690
Jung et al (2008) Reactive oxygen species stabilize hypoxia-inducible factor-1 alpha protein and stimulate transcriptional activity via AMP-activated protein kinase in DU145 human prostate cancer cells. Carcinogenesis 29 713 PMID: 18258605
Gross et al (2006) The JAK/STAT pathway is essential for opioid-induced cardioprotection: JAK2 as a mediator of STAT3, Akt, and GSK-3 beta. Am J Physiol Heart Circ Physiol 291 H827 PMID: 16517948
Bellik et al (2005) Intracellular pathways triggered by the selective FLT-1-agonist placental growth factor in vascular smooth muscle cells exposed to hypoxia. Br J Pharmacol 146 568 PMID: 16086034
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