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Submit ReviewTucatinib 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. 了解 Tocris 化合物库的更多信息。
分子量 | 480.52 |
公式 | C26H24N8O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 937263-43-9 |
PubChem ID | 51039094 |
InChI Key | SDEAXTCZPQIFQM-UHFFFAOYSA-N |
Smiles | N=1C=NC(NC2=CC=C(OC=3C=CN4N=CN=C4C3)C(=C2)C)=C5C=C(C=CC15)NC6=NC(C)(C)CO6 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 48.05 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for Tucatinib, please let us know.
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