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Tyrphostin AG 1478

EGFR inhibitor
ALX-270-036-M001 1 mg 34.00 USD
ALX-270-036-M005 5 mg 93.00 USD
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Replaces Prod. #: BML-EI277

Potent and selective inhibitor of EGFR (IC50 = 3nM). Reduces EGF-stimulated DNA synthesis in Rat-1 fibroblasts by ~75% at 0.25μM. Blocks EGF-dependent src-family kinase activation and p21/Cip 1/WAF1 induction in A431 cells. Also inhibits H2O2-induced stimulation of amphiregulin expression in rat gastric epithelium (RGM 1) cells.

Product Specification

Alternative Name:4-(3-Chloroanilino)-6,7-dimethoxyquinazoline
Purity:≥98% (HPLC)
Appearance:White to light yellow solid.
Solubility:Soluble in DMSO (10mg/ml).
Long Term Storage:-20°C
Handling:Protect from light. Packaged under inert gas.
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Product Literature References

Regulation of the hyperosmotic induction of aquaporin 5 and VEGF in retinal pigment epithelial cells: involvement of NFAT5: M. Hollborn, et al.; Mol. Vis. 21, 360 (2015), Application(s): Cell Culture, Abstract; Full Text
Ectopic expression of B-lymphoid kinase in cutaneous T-cell lymphoma: T. Krejsgaard, et al.; Blood 113, 5896 (2009), Abstract;
Apoptosis and growth inhibition of head and neck tumor cell line induced by epidermal growth factor receptor tyrosine kinase inhibitor: R.A. Faust, et al.; Oral Oncol. 35, 290 (1999), Abstract;
Inhibition of epidermal-growth-factor-receptor-dependent signalling by tyrphostins A25 and AG1478 blocks growth and induces apoptosis in colorectal tumor cells in vitro: G. Partik, et al.; J. Cancer Res. Clin. Oncol. 125, 379 (1999), Abstract;
Inhibition of epidermal growth factor receptor kinase induces protease- dependent apoptosis in human colon cancer cells: W.E. Karnes, et al.; Gastroenterology 114, 930 (1998), Abstract;
Role of heparin-binding EGF-related peptides in proliferation and apoptosis of activated ras-stimulated intestinal epithelial cells: S. Zushi, et al.; Int. J. Cancer 73, 917 (1997), Abstract;
Oxidative stress increases gene expression of heparin-binding EGF-like growth factor and amphiregulin in cultured rat gastric epithelial cells: Y. Miyazaki, et al.; BBRC 226, 542 (1996), Abstract;
Role of transactivation of the EGF receptor in signalling by G-protein-coupled receptors: H. Daub, et al.; Nature 379, 557 (1996), Abstract;
Prolonged induction of p21Cip1/WAF1/CDK2/PCNA complex by epidermal growth factor receptor activation mediates ligand-induced A431 cell growth inhibition: Z. Fan, et al.; J. Cell Biol. 131, 235 (1995), Abstract;
Tyrosine kinase inhibition: an approach to drug development: A. Levitzki & A. Gazit; Science 267, 1782 (1995), Abstract;
Epidermal-growth-factor-dependent activation of the src-family kinases: N. Osherov & A. Levitzki; Eur. J. Biochem. 225, 1047 (1994), Abstract;

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