FAK Inhibitor 14 is a selective focal adhesion kinase (FAK) inhibitor, it prevents FAK autophosphorylation at Y397 (IC50 = 1μM).
FAK Inhibitor 14 displays no significant activity at a range of other kinases including EGFR, PDGFR and IGF-RI. FAK Inhibitor 14 promotes cell detachment and inhibits cell adhesion in vitro, and exhibits antiproliferative activity in a variety of human tumor cell lines in vitro and in breast cancer cells in vivo.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Hochwald et al (2009) A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle 8 2435. PMID: 19571674.
[2] Golubovskaya et al (2008) A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the Y397 site of focal adhesion kinase decreases tumour growth. J.Med.Chem. 51 7405. PMID: 18989950.
[3] Thordarson, P., et al. 2003. Org. Biomol. Chem. 1: 1216-1225. PMID: 12926398
[4] Beierle, E.A., et al. 2010. Cell Cycle. 9: 1005-1015. PMID: 20160475
分子式 C6H14Cl4N4 |
分子量 284.01 |
CAS号 4506-66-5 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 75 mM |
Water 20 mM |
Ethanol 5 mM |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02758587 | Carcinoma, Non-small-cell Lung|Mesothelioma|Pancreatic Neoplasms | Drug: Defactinib|Drug: Pembrolizumab | NHS Greater Glasgow and Clyde|University of Glasgow|Cancer Research UK|Merck Sharp & Dohme Corp.|Verastem, Inc.|University of Edinburgh|University of Southampton|University of Leicester|Queen's University, Belfast | Phase 1|Phase 2 | 2016-06-01 | 2016-06-14 |
NCT00666926 | Head and Neck Neoplasm|Prostatic Neoplasm|Pancreatic Neoplasm | Drug: PF00562271|Drug: PF00562271|Drug: PF00562271|Drug: PF00562271 | Verastem, Inc. | Phase 1 | 2005-12-01 | 2013-03-14 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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