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Tyrphostin AG 1478

ALX-270-036

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EGFR inhibitor

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.

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Product Details

Alternative Name	4-(3-Chloroanilino)-6,7-dimethoxyquinazoline
Appearance	White to light yellow solid.
CAS	153436-53-4
Couple Target	EGFR
Couple Type	Inhibitor
Formula	C₁₆H₁₄ClN₃O₂
MW	315.8
Purity	≥98% (HPLC)
Solubility	Soluble in DMSO (10mg/ml).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Handling	Protect from light. Packaged under inert gas.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Osmotic regulation of aquaporin-8 expression in retinal pigment epithelial cells in vitro: Dependence on KATP channel activation: B. Schnabel, et al.; Mol. Vis. 26, 797 (2020), Abstract
Neuregulin-1 is a chemoattractant and chemokinetic molecule for trunk neural crest cells: de Bellard, M. E., Ortega, B., et al.; Dev. Dyn. 247, 888 (2018), Abstract
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
IL-15 and IL-17F are differentially regulated and expressed in mycosis fungoides (MF): Willerslev-Olsen, A., Litvinov, I. V., et al.; Cell Cycle 13, 1306 (2014), Abstract
Ectopic expression of B-lymphoid kinase in cutaneous T-cell lymphoma: T. Krejsgaard, et al.; Blood 113, 5896 (2009), Abstract
Preconditioning-mimetics bradykinin and DADLE activate PI3-kinase through divergent pathways: Cohen, M. V., Philipp, S., et al.; J. Mol. Cell. Cardiol. 42, 842 (2007), 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
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 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

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Tyrphostin AG 1478

ALX-270-036

Product Details

Handling & Storage

Datasheet, Manuals, SDS & CofA

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