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Submit ReviewTAK 165 is a 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.
分子量 | 468.47 |
公式 | C25H23F3N4O2 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 366017-09-6 |
PubChem ID | 6444692 |
InChI Key | ZTFBIUXIQYRUNT-MDWZMJQESA-N |
Smiles | FC(C(C=C2)=CC=C2/C=C/C1=NC(COC3=CC=C(CCCCN4C=CN=N4)C=C3)=CO1)(F)F |
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 | 35.14 | 75 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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 PMID: 16771730
Spector et al (2007) Small molecule HER-2 tyrosine kinase inhibitors. Breast Cancer Res. 9 205
If you know of a relevant reference for TAK 165, please let us know.
关键词: 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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