AG 490

Pricing Availability Delivery Time Qty
Cat.No. 0414 - AG 490 | C17H14N2O3 | CAS No. 133550-30-8
Description: EGFR-kinase inhibitor. Also JAK2, JAK3 inhibitor
Alternative Names: Tyrphostin AG 490
Chemical Name: (E)-2-Cyano-3-(3,4-dihydrophenyl)-N-(phenylmethyl)-2-propenamide
Purity: ≥99% (HPLC)
Datasheet
Citations (8)
Reviews
Literature

Biological Activity

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.

Technical Data

M. Wt 294.31
Formula C17H14N2O3
Storage Store at RT
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 29.43 100
ethanol 5.89 20

Preparing Stock Solutions

The following data is based on the product molecular weight 294.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 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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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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.

View Related Products by Product Action

View all EGFR Inhibitors

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8 Citations for AG 490

Citations are publications that use Tocris products. Selected citations for AG 490 include:

Tactacan et al (2015) The pseudokinase SgK223 promotes invasion of pancreatic ductal epithelial cells through JAK1/Stat3 signaling. Mol Cancer 14 139 PMID: 26215634

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

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

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

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


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