AP26113, A POTENT ALK INHIBITOR, IS ALSO ACTIVE AGAINST EGFR T790M IN MOUSE MODELS OF NSCLC

被引:0
|
作者
Miret, Juan J. [1 ]
Wang, Frank [1 ]
Anjum, Rana [1 ]
Zhang, Sen [1 ]
Keats, Jeffrey [1 ]
Cookson, Michelle [1 ]
Ning, Yaoyu [1 ]
Wardwell, Scott [1 ]
Moran, Lauren [1 ]
Mohemmad, Qurish [1 ]
Wang, Yihan [1 ]
Qi, Jiwei [1 ]
Squillace, Rachel [1 ]
Narasimhan, Narayana [1 ]
Dalgarno, David [1 ]
Clackson, Tim [1 ]
Shakespeare, William [1 ]
Rivera, Victor [1 ]
机构
[1] ARIAD Pharmaceut Inc, Biol, Cambridge, MA USA
关键词
EGFR T790M; reversible kinase inhibitor; AP26113; ALK;
D O I
暂无
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
引用
收藏
页码:S577 / S578
页数:2
相关论文
共 50 条
  • [1] AP26113 is a dual ALK/EGFR inhibitor: Characterization against EGFR T790M in cell and mouse models of NSCLC
    Rivera, Victor M.
    Wang, Frank
    Anjum, Rana
    Zhang, Sen
    Squillace, Rachel
    Keats, Jeffrey
    Miller, David
    Ning, Yaoyu
    Wardwell, Scott D.
    Moran, Lauren
    Miret, Juan
    Narasimhan, Narayana
    Dalgarno, David
    Clackson, Tim
    Shakepeare, William C.
    CANCER RESEARCH, 2012, 72
  • [2] Discovery of a potent dual ALK and EGFR T790M inhibitor
    Jang, Jaebong
    Son, Jung Beom
    To, Ciric
    Bahcall, Magda
    Kim, So Young
    Kang, Seock Yong
    Mushajiang, Mierzhati
    Lee, Younho
    Janne, Pasi A.
    Choi, Hwan Geun
    Gray, Nathanael S.
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2017, 136 : 497 - 510
  • [3] The Dual ALK/EGFR Inhibitor AP26113 Also Potently Inhibits Activated and Gatekeeper Mutant Forms of ROS1
    Anjum, R.
    Zhang, S.
    Squillace, R.
    Clackson, T.
    Garner, A. P.
    Rivera, V. M.
    EUROPEAN JOURNAL OF CANCER, 2012, 48 : 50 - 50
  • [4] The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models
    Zhang, Sen
    Anjum, Rana
    Squillace, Rachel
    Nadworny, Sara
    Zhou, Tianjun
    Keats, Jeff
    Ning, Yaoyu
    Wardwell, Scott D.
    Miller, David
    Song, Youngchul
    Eichinger, Lindsey
    Moran, Lauren
    Huang, Wei-Sheng
    Liu, Shuangying
    Zou, Dong
    Wang, Yihan
    Mohemmad, Qurish
    Jang, Hyun Gyung
    Ye, Emily
    Narasimhan, Narayana
    Wang, Frank
    Miret, Juan
    Zhu, Xiaotian
    Clackson, Tim
    Dalgarno, David
    Shakespeare, William C.
    Rivera, Victor M.
    CLINICAL CANCER RESEARCH, 2016, 22 (22) : 5527 - 5538
  • [5] TAS-2913 is a Mutant Selective EGFR Inhibitor for NSCLC: Characterization Against EGFR T790M in Cell and Xenograft Models
    Miyadera, K.
    Kato, M.
    Takahashi, I.
    Ito, K.
    Aoyagi, Y.
    Fukasawa, K.
    Sagara, T.
    Yonekura, K.
    Iwasawa, Y.
    Utsugi, T.
    EUROPEAN JOURNAL OF CANCER, 2012, 48 : 44 - 44
  • [6] The potent ALK inhibitor AP26113 can overcome mechanisms of resistance to first- and second-generation ALK TKIs in preclinical models
    Zhang, Sen
    Nadworny, Sara
    Wardwell, Scott D.
    Eichinger, Lindsey
    Das, Biplab
    Ye, Emily Y.
    Hodgson, J. Graeme
    Rivera, Victor M.
    CANCER RESEARCH, 2015, 75
  • [7] Discovery of AP26113, a potent, orally active inhibitor of anaplastic lymphoma kinase and clinically relevant mutants
    Huang, Wei-Sheng
    Li, Feng
    Cai, Lisi
    Xu, Yongjin
    Zhang, Sen
    Wardwell, Scott D.
    Ning, Yaoyu
    Kohlmann, Anna
    Zhou, Tianjun
    Ye, Emily Y.
    Zhu, Xiaotian
    Narasimhan, Narayana I.
    Clackson, Tim
    Rivera, Victor M.
    Dalgarno, David
    Shakespeare, William C.
    CANCER RESEARCH, 2015, 75
  • [8] A FIRST-IN-HUMAN DOSE-FINDING STUDY OF THE ALK/EGFR INHIBITOR AP26113 IN PATIENTS WITH ADVANCED MALIGNANCIES
    Gettinger, S.
    Weiss, G. J.
    Salgia, R.
    Bazhenova, L.
    Narasimhan, N. I.
    Dorer, J.
    Rivera, V. M.
    Zhang, J.
    Clackson, T.
    Haluska, F.
    Shaw, A. T.
    Camidge, D. R.
    ANNALS OF ONCOLOGY, 2012, 23 : 152 - 152
  • [9] Molecular dynamics and pharmacophore modelling studies of different subtype (ALK and EGFR (T790M)) inhibitors in NSCLC
    Singh, P. K.
    Silakari, O.
    SAR AND QSAR IN ENVIRONMENTAL RESEARCH, 2017, 28 (03) : 221 - 233
  • [10] Amplification of EGFR T790M causes resistance to an irreversible EGFR inhibitor
    D Ercan
    K Zejnullahu
    K Yonesaka
    Y Xiao
    M Capelletti
    A Rogers
    E Lifshits
    A Brown
    C Lee
    J G Christensen
    D J Kwiatkowski
    J A Engelman
    P A Jänne
    Oncogene, 2010, 29 : 2346 - 2356