AG 490

Pricing Availability   Qty
说明: EGFR-kinase inhibitor. Also JAK2, JAK3 inhibitor
别名: Tyrphostin AG 490
化学名: (E)-2-Cyano-3-(3,4-dihydrophenyl)-N-(phenylmethyl)-2-propenamide
纯度: ≥99% (HPLC)
说明书
引用文献 (14)
评论
文献 (1)

生物活性 for AG 490

AG 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.

技术数据 for AG 490

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.

溶解性数据 for AG 490

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
ethanol 5.89 20
DMSO 29.43 100

制备储备液 for AG 490

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.

选择批次从而根据批次分子量重新计算:
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

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产品说明书 for AG 490

分析证书/产品说明书
选择另一批次:

参考文献 for AG 490

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.

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查看全部 EGFR Inhibitors

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

14 篇 AG 490 的引用文献

引用文献是使用了 Tocris 产品的出版物。 AG 490 的部分引用包括:

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

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

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

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

Azad et al (2017) PD-L1 blockade enhances response of pancreatic ductal adenocarcinoma to radiotherapy. EMBO Mol Med 9 167 PMID: 27932443

Doulatov et al (2009) PLZF is a regulator of homeostatic and cytokine-induced myeloid development. Genes Dev 23 2076 PMID: 19723763

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

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

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


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