Home > FAK & FAK & > Defactinib

Defactinib

VS-6063,PF-04554878

Defactinib (VS-6063, PF-04554878) 是选择性且口服具有活性的FAK激酶磷酸化抑制剂,能通过AKY依赖性通路以克服YB1介导的paclitaxel耐受,Phase 2。

目录号
EY0796
EY0796
EY0796
EY0796
纯度
99.53%
99.53%
99.53%
99.53%
规格
5 mg
10 mg
25 mg
50 mg
原价
758.00_
1,168.00_
2020
2860
售价
758.00_
1,168.00_
2020
2860
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Defactinib inhibited FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. The combination of VS-6063 and paclitaxel markedly decreased proliferation and increased apoptosis, which resulted in 92.7% to 97.9% reductions in tumor weight. FAK inhibition enhanced chemosensitivity in taxane-resistant cells by decreasing YB-1 phosphorylation and subsequently CD44 in an AKT-dependent manner.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~10 μM

  • 动物实验

    50 mg/kgp.o.

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm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。


  • 参考文献

    [1] Kang Y, et al. Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95.

    分子式
    C20H21F3N8O3S
    分子量
    510.49
    CAS号
    1073154-85-4
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    5 mg/mL
    Water
    <1 mg/mL
    Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02913716 Healthy Subjects Drug: defactinib Verastem, Inc. Phase 1 2015-08-01 2017-01-26
    NCT02943317 Epithelial Ovarian Cancer Drug: Part A - VS-6063|Drug: Part A - Avelumab Verastem, Inc. Phase 1 2016-10-01 2017-01-30
    NCT02004028 Malignant Pleural Mesothelioma Drug: VS-6063 Verastem, Inc. Phase 2 2013-12-01 2017-02-01
    NCT01943292 Non Hematologic Cancers Drug: Defactinib Verastem, Inc. Phase 1 2013-09-02 2017-01-26
    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
    NCT01870609 Malignant Pleural Mesothelioma Drug: defactinib (VS-6063)|Drug: Placebo Verastem, Inc. Phase 2 2013-09-01 2017-01-26
    NCT02546531 Advanced Solid Tumors|Solid Tumors|Pancreatic Cancer Biological: Defactinib|Biological: Pembrolizumab|Drug: Gemcitabine Washington University School of Medicine Phase 1 2016-02-03 2017-02-22
    NCT01778803 Ovarian Cancer Drug: defactinib (VS-6063)|Drug: Paclitaxel Verastem, Inc. Phase 1 2013-01-01 2015-06-01
    NCT01951690 Non Small Cell Lung Cancer|Lung Cancer Drug: defactinib (VS-6063) Verastem, Inc. Phase 2 2013-09-01 2017-02-01

    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。

  • 相关化合物库

  • 使用AMQUAR产品发表文献后请联系我们

相关推荐

X
  • 联系人 :
  • 收件地址 :
  • 电话号码 :
  • 单位名称 :
  • 产品货号 :
  • 产品规格 :
  • 发票抬头以及单位税号 :