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Cat. No. Name Size Price Add Cart
KI0514AG-14785 mg$112
AG-147810 mg$176
AG-147825 mg$352
AG-147850 mg$592

Chemical Characteristic

Product NameAG-1478
SynonymsTyrphostin AG-1478
CAS No.153436-53-4
Molecular Weight 315.75
FormulaC16H14ClN3O2
Chemical NameN-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine
Smilesn1cnc(c2cc(c(cc12)OC)OC)Nc1cc(ccc1)Cl
Chemical Structure

Biological activities

AG-1478 is an inhibitor of the EGFR tyrosine kinase. AG-1478 inhibits the EGFR kinase with an IC50 of 3 nM. AG-1478 induces expression of Bak and down-regulates Bcl-2. AG-1478 inhibits DNA synthesis and induces cell loss in colorectal tumor cells in vitro. AG-1478 effectively induces apoptosis in all tumor cell lines (SW480 and T84 colon carcinoma cells).[1] AG-1478 rapidly and reversibly inhibits Kv1.5 currents at 50 mV, with an IC50 of 9.82 mM. AG-1478 accelerates the decay rate of inactivation of Kv1.5 currents without modifying the kinetics of current activation. [2] AG-1478 abolishes the mitogen-activated protein kinase (MAPK) activation induced by Ang II, a Ca2+ ionophore as well as EGF. [3] Parenteral administration of soluble AG-1478 blocks phosphorylation of the EGFR at the tumor site and inhibits the growth of A431 xenografts. [4]

Protocols

AG-1478 is dissolved in DMSO to yield stock solution of 50 mM. [2]

References

[1] Partik G, et al. Inhibition of epidermal-growth-factor-receptor-dependent signalling by tyrphostins A25 and AG1478 blocks growth and induces apoptosis in colorectal tumor cells in vitro. J Cancer Res Clin Oncol. 1999, 125(7): 379-388.
[2] Choi BH, et al. Direct inhibition of the cloned Kv1.5 channel by AG-1478, a tyrosine kinase inhibitor. Am J Physiol Cell Physiol. 2002, 282(6): C1461-1468.
[3] Eguchi S, et al. Calcium-dependent epidermal growth factor receptor transactivation mediates the angiotensin II-induced mitogen-activated protein kinase activation in vascular smooth muscle cells. J Biol Chem. 1998, 273(15): 8890-8896.
[4] Johns TG, et al. Antitumor efficacy of cytotoxic drugs and the monoclonal antibody 806 is enhanced by the EGF receptor inhibitor AG1478. Proc Natl Acad Sci U S A. 2003, 100(26): 15871-15876.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

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