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 TAE684

NVP-TAE684 is  a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC(50) values between 2 and 10 nM. NVP-TAE684 treatment resulted in a rapid and sustained inhibition of phosphorylation of NPM-ALK and its downstream effectors and subsequent induction of apoptosis and cell cycle arrest. In vivo, NVP-TAE684 suppressed lymphomagenesis in two independent models of ALK-positive ALCL and induced regression of established Karpas-299 lymphomas. NVP-TAE684 also induced down-regulation of CD30 expression, suggesting that CD30 may be used as a biomarker of therapeutic NPM-ALK kinase activity inhibition. (source:  http://www.ncbi.nlm.nih.gov/pubmed/17185414).

Current developer:   Genomics Institute of the Novartis Research Foundation

NVP-TAE684 is  a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC(50) values between 2 and 10 nM. NVP-TAE684 treatment resulted in a rapid and sustained inhibition of phosphorylation of NPM-ALK and its downstream effectors and subsequent induction of apoptosis and cell cycle arrest. In vivo, NVP-TAE684 suppressed lymphomagenesis in two independent models of ALK-positive ALCL and induced regression of established Karpas-299 lymphomas. NVP-TAE684 also induced down-regulation of CD30 expression, suggesting that CD30 may be used as a biomarker of therapeutic NPM-ALK kinase activity inhibition. see http://www.ncbi.nlm.nih.gov/pubmed/17185414.

Current developer:   Genomics Institute of the Novartis Research Foundation

 1. McDermott, Ultan; Pusapati, Raju V.; Christensen, James G.; Gray, Nathanael S.; Settleman, Jeff. Acquired Resistance of Non-Small Cell Lung Cancer Cells to MET Kinase Inhibition Is Mediated by a Switch to Epidermal Growth Factor Receptor Dependency. Cancer Research (2010), 70(4), 1625-1634. 

2. Lee, Charles; Murphy, Carly; Janne, Pasi. FISH assay for echinoderm microtubule-associated protein-like 4 (EML4) and anaplastic lymphoma kinase (ALK) gene chromosomal inversion in lung cancer. PCT Int. Appl. (2009), 64pp. CODEN: PIXXD2 WO 2009102446 A2 20090820 

3. Mcdermott, Ultan; Sharma, Sreenath V.; Dowell, Lori; Greninger, Patricia; Montagut, Clara; Lamb, Jennifer; Archibald, Heidi; Raudales, Raul; Tam, Angela; Lee, Diana; Rothenberg, S. Michael; Supko, Jeffrey G.; Sordella, Raffaella; Ulkus, Lindsey E.; Lafrate, A. John; Maheswaran, Shyamala; Njauw, Ching Ni; Tsao, Hensin; Drew, Lisa; Hanke, Jeff H.; Ma, Xiao-Jun; Erlander, Mark G.; Gray, Nathanael S.; Haber, Daniel A.; Settleman, Jeffrey. Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proceedings of the National Academy of Sciences of the United States of America (2007), 104(50), 19936-19941. 

4. Galkin, Anna V.; Melnick, Jonathan S.; Kim, Sungjoon; Hood, Tami L.; Li, Nanxin; Li, Lintong; Xia, Gang; Steensma, Ruo; Chopiuk, Greg; Jiang, Jiqing; Wan, Yongqin; Ding, Peter; Liu, Yi; Sun, Fangxian; Schultz, Peter G.; Gray, Nathanael S.; Warmuth, Markus. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. [Erratum to document cited in CA146:308635]. Proceedings of the National Academy of Sciences of the United States of America (2007), 104(6), 2025. 

5. Galkin, Anna V.; Melnick, Jonathon S.; Kim, Sunjoon; Hood, Tami L.; Li, Nanxin; Li, Lintong; Xia, Gang; Steensma, Ruo; Chopiuk, Greg; Wan, Yongqin; Ding, Peter; Liu, Yi; Sun, Fangxian; Schultz, Peter G.; Gray, Nathanael S.; Warmuth, Markus. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proceedings of the National Academy of Sciences of the United States of America (2007), 104(1), 270-275. 

6. Schonherr C; Yang H-L; Vigny M; Palmer R H; Hallberg B Anaplastic lymphoma kinase activates the small GTPase Rap1 via the Rap1-specific GEF C3G in both neuroblastoma and PC12 cells. Oncogene (2010), 29(19), 2817-30.

7. McDermott Ultan; Iafrate A John; Gray Nathanael S; Shioda Toshi; Classon Marie; Maheswaran Shyamala; Zhou Wenjun; Choi Hwan Geun; Smith Shannon L; Dowell Lori; Ulkus Lindsey E; Kuhlmann Georgiana; Greninger Patricia; Christensen James G; Haber Daniel A; Settleman Jeffrey Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer research (2008), 68(9), 3389-95.