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Potent, irreversible human epithelial growth factor receptor 2 (ErbB2) inhibitor (IC50 = 6 nM) that displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Exhibits potent antiproliferative effects in ErbB2-overexpressing cancer cell lines (IC50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth in vivo.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 468.47. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.75 mM||2.85 mL||14.23 mL||28.46 mL|
|3.75 mM||0.57 mL||2.85 mL||5.69 mL|
|7.5 mM||0.28 mL||1.42 mL||2.85 mL|
|37.5 mM||0.06 mL||0.28 mL||0.57 mL|
References are publications that support the biological activity of the product.
Sridhar et al (2003) Inhibitors of epidermal-growth-factor receptors: a review of clinical research with a focus on non-small-cell lung cancer. Lancet Oncol. 4 397 PMID: 12850190
Nagasawa et al (2006) Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. Int.J.Urol. 13 585
Spector et al (2007) Small molecule HER-2 tyrosine kinase inhibitors. Breast Cancer Res. 9 205
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Keywords: TAK 165, TAK 165 supplier, Potent, selective, ErbB2, inhibitors, inhibits, Epidermal, Growth, Factor, Receptors, Her, EGFR, Receptor, Tyrosine, Kinases, RTKs, TAK165, Mubritinib, 3599, Tocris Bioscience
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Literature in this Area
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Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.