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Tucatinib is a potent and selective ErbB-2 (also called HER2) kinase inhibitor (IC50 = 7 nM). It exhibits >50-fold selectivity for ErbB-2 over EGFR. In vitro, Tucatinib inhibits ErbB-2 signaling activity and cell proliferation in ErbB-2-amplified breast cancer cell lines (BT-474). In vivo, Tucatinib (25-100 mg/kg) reduces tumor volume in breast and gastric xenograft mouse models.This compound is orally bioavailable.
Tucatinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°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|
The following data is based on the product molecular weight 480.52. 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|
|1 mM||2.08 mL||10.41 mL||20.81 mL|
|5 mM||0.42 mL||2.08 mL||4.16 mL|
|10 mM||0.21 mL||1.04 mL||2.08 mL|
|50 mM||0.04 mL||0.21 mL||0.42 mL|
References are publications that support the biological activity of the product.
Kulukian et al (2020) Preclinical activity of HER2-selective Tyrosine Kinase inhibitor Tucatinib as a single agent or in combination with Trastuzumab or Docetaxel in solid tumor models. Mol.Cancer.Ther. 19 976 PMID: 32241871
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Keywords: Tucatinib, Tucatinib supplier, Potent, selective, ErbB2, HER2, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, ErbB, Her, EGFR, Receptor, Tyrosine, Kinases, orally, bioavailable, 7640, Tocris Bioscience
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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.