Defactinib
货号:
17737-1mg 基本售价:
406.0 元 规格:
1 mg
产品信息
概述货号 | 17737-1mg |
描述 | Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that plays a vital role in many oncogenic pathways.1,2 Defactinib is a dose-dependent inhibitor of FAK, with maximal inhibition of FAK autophosphorylation in cells achieved at 10 µM.3 It is less effective against the related kinase PYK2. Defactinib restores the chemosensitivity of taxane-resistant cells to paclitaxel (Item No. 10461), although it is not cytotoxic alone.3 Defactinib decreases YB-1 phosphorylation and nuclear accumulation in an Akt-dependent manner. It is orally bioavailable, inhibiting FAK and augmenting paclitaxel action in suppressing the growth and number of ovarian cancer cell tumors in mice.3 |
别名 | PF-04554878;VS-6063; |
性能供应商 | Cayman |
应用文献 |
1.Schwock, J.,Dhani, N. and Hedley, D.W. Targeting focal adhesion kinase signaling in tumor growth and metastasis. Expert Opin.Ther.Targets 14(1), 77-94 (2010). 2.Lee, B.Y.,Timpson, P.,Horvath, L.G., et al. FAK signaling in human cancer as a target for therapeutics. Pharmacology & Therapeutics 146, 132-149 (2015). 3.Kang, Y.,Hu, W.,Ivan, C., et al. Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer. JNCI 105, 1485-1495 (2013).
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运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 510.5 |
分子式 | C20H21F3N8O3S |
CAS号 | 1073154-85-4 |
稳定性 | ≥ 2 years |
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