The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

Dasatinib     N-(2-chloro-6-methyl-phenyl)- 2-[[6-[4-(2...

Synonyms: Sprycel, Spyrcel, dasatinibum, Dasatinib;, AmbotzLS-1203, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of Dasatinib


High impact information on Dasatinib


Chemical compound and disease context of Dasatinib


Biological context of Dasatinib


Anatomical context of Dasatinib


Associations of Dasatinib with other chemical compounds

  • 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor [18].
  • The presence of BCR-ABL mutations conferring imatinib resistance did not preclude a response to dasatinib [20].
  • At the molecular level, Dasatinib significantly counteracted the Nutlin-3-mediated induction of the p53 transcriptional targets MDM2 and p21 observed in p53(wild-type) leukemic cells [21].
  • Pharmacodynamic studies indicated apoptosis in peripheral blood CLL cells within 3 to 6 hours after dasatinib administration, associated with downregulation of Syk (spleen tyrosine kinase) mRNA [22].
  • Due to the high incidence of myelosuppression with subsequent cycles, the recommended phase II dose of dasatinib is 150 mg daily in combination with paclitaxel and carboplatin [23].
  • We show that high levels of CAV-1, EphA2 phosphorylation at S897, and the status of PTEN are key determinants of dasatinib response in uterine carcinoma [24].

Gene context of Dasatinib


  1. Dasatinib (BMS-354825) is active in Philadelphia chromosome-positive chronic myelogenous leukemia after imatinib and nilotinib (AMN107) therapy failure. Quintas-Cardama, A., Kantarjian, H., Jones, D., Nicaise, C., O'brien, S., Giles, F., Talpaz, M., Cortes, J. Blood (2007) [Pubmed]
  2. Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis. Shah, N.P., Lee, F.Y., Luo, R., Jiang, Y., Donker, M., Akin, C. Blood (2006) [Pubmed]
  3. Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Song, L., Morris, M., Bagui, T., Lee, F.Y., Jove, R., Haura, E.B. Cancer Res. (2006) [Pubmed]
  4. Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. Nam, S., Kim, D., Cheng, J.Q., Zhang, S., Lee, J.H., Buettner, R., Mirosevich, J., Lee, F.Y., Jove, R. Cancer Res. (2005) [Pubmed]
  5. Identification of candidate molecular markers predicting sensitivity in solid tumors to dasatinib: rationale for patient selection. Huang, F., Reeves, K., Han, X., Fairchild, C., Platero, S., Wong, T.W., Lee, F., Shaw, P., Clark, E. Cancer Res. (2007) [Pubmed]
  6. Profound inhibition of antigen-specific T-cell effector functions by dasatinib. Weichsel, R., Dix, C., Wooldridge, L., Clement, M., Fenton-May, A., Sewell, A.K., Zezula, J., Greiner, E., Gostick, E., Price, D.A., Einsele, H., Seggewiss, R. Clin. Cancer Res. (2008) [Pubmed]
  7. Characteristics of dasatinib- and imatinib-resistant chronic myelogenous leukemia cells. Okabe, S., Tauchi, T., Ohyashiki, K. Clin. Cancer Res. (2008) [Pubmed]
  8. Inhibition of SRC family kinases and receptor tyrosine kinases by dasatinib: possible combinations in solid tumors. Montero, J.C., Seoane, S., Ocaña, A., Pandiella, A. Clin. Cancer Res. (2011) [Pubmed]
  9. A phase 2 trial of dasatinib in patients with advanced HER2-positive and/or hormone receptor-positive breast cancer. Mayer, E.L., Baurain, J.F., Sparano, J., Strauss, L., Campone, M., Fumoleau, P., Rugo, H., Awada, A., Sy, O., Llombart-Cussac, A. Clin. Cancer Res. (2011) [Pubmed]
  10. Dasatinib as a single agent in triple-negative breast cancer: results of an open-label phase 2 study. Finn, R.S., Bengala, C., Ibrahim, N., Roché, H., Sparano, J., Strauss, L.C., Fairchild, J., Sy, O., Goldstein, L.J. Clin. Cancer Res. (2011) [Pubmed]
  11. Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance. Burgess, M.R., Skaggs, B.J., Shah, N.P., Lee, F.Y., Sawyers, C.L. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  12. Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)-based mutagenesis screen: high efficacy of drug combinations. Bradeen, H.A., Eide, C.A., O'hare, T., Johnson, K.J., Willis, S.G., Lee, F.Y., Druker, B.J., Deininger, M.W. Blood (2006) [Pubmed]
  13. Leukemogenesis induced by wild-type and STI571-resistant BCR/ABL is potently suppressed by C/EBPalpha. Ferrari-Amorotti, G., Keeshan, K., Zattoni, M., Guerzoni, C., Iotti, G., Cattelani, S., Donato, N.J., Calabretta, B. Blood (2006) [Pubmed]
  14. Dasatinib (BMS-354825) targets an earlier progenitor population than imatinib in primary CML but does not eliminate the quiescent fraction. Copland, M., Hamilton, A., Elrick, L.J., Baird, J.W., Allan, E.K., Jordanides, N., Barow, M., Mountford, J.C., Holyoake, T.L. Blood (2006) [Pubmed]
  15. Cotreatment with Vorinostat (Suberoylanilide Hydroxamic Acid) Enhances Activity of Dasatinib (BMS-354825) against Imatinib Mesylate-Sensitive or Imatinib Mesylate-Resistant Chronic Myelogenous Leukemia Cells. Fiskus, W., Pranpat, M., Balasis, M., Bali, P., Estrella, V., Kumaraswamy, S., Rao, R., Rocha, K., Herger, B., Lee, F., Richon, V., Bhalla, K. Clin. Cancer Res. (2006) [Pubmed]
  16. Dasatinib inhibits migration and invasion in diverse human sarcoma cell lines and induces apoptosis in bone sarcoma cells dependent on SRC kinase for survival. Shor, A.C., Keschman, E.A., Lee, F.Y., Muro-Cacho, C., Letson, G.D., Trent, J.C., Pledger, W.J., Jove, R. Cancer Res. (2007) [Pubmed]
  17. Dasatinib (BMS-354825) Pharmacokinetics and Pharmacodynamic Biomarkers in Animal Models Predict Optimal Clinical Exposure. Luo, F.R., Yang, Z., Camuso, A., Smykla, R., McGlinchey, K., Fager, K., Flefleh, C., Castaneda, S., Inigo, I., Kan, D., Wen, M.L., Kramer, R., Blackwood-Chirchir, A., Lee, F.Y. Clin. Cancer Res. (2006) [Pubmed]
  18. 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor. Das, J., Chen, P., Norris, D., Padmanabha, R., Lin, J., Moquin, R.V., Shen, Z., Cook, L.S., Doweyko, A.M., Pitt, S., Pang, S., Shen, D.R., Fang, Q., de Fex, H.F., McIntyre, K.W., Shuster, D.J., Gillooly, K.M., Behnia, K., Schieven, G.L., Wityak, J., Barrish, J.C. J. Med. Chem. (2006) [Pubmed]
  19. Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib). Chen, Z., Lee, F.Y., Bhalla, K.N., Wu, J. Mol. Pharmacol. (2006) [Pubmed]
  20. Dasatinib induces rapid hematologic and cytogenetic responses in adult patients with Philadelphia chromosome positive acute lymphoblastic leukemia with resistance or intolerance to imatinib: interim results of a phase 2 study. Ottmann, O., Dombret, H., Martinelli, G., Simonsson, B., Guilhot, F., Larson, R.A., Rege-Cambrin, G., Radich, J., Hochhaus, A., Apanovitch, A.M., Gollerkeri, A., Coutre, S. Blood (2007) [Pubmed]
  21. Dasatinib Plus Nutlin-3 Shows Synergistic Antileukemic Activity in Both p53wild-type and p53mutated B Chronic Lymphocytic Leukemias by Inhibiting the Akt Pathway. Zauli, G., Voltan, R., Bosco, R., Melloni, E., Marmiroli, S., Rigolin, G.M., Cuneo, A., Secchiero, P. Clin. Cancer Res. (2011) [Pubmed]
  22. Phase II Study of Dasatinib in Relapsed or Refractory Chronic Lymphocytic Leukemia. Amrein, P.C., Attar, E.C., Takvorian, T., Hochberg, E.P., Ballen, K.K., Leahy, K.M., Fisher, D.C., Lacasce, A.S., Jacobsen, E.D., Armand, P., Hasserjian, R.P., Werner, L., Neuberg, D., Brown, J.R. Clin. Cancer Res. (2011) [Pubmed]
  23. A phase I trial of dasatinib, an SRC-family kinase inhibitor, in combination with Paclitaxel and Carboplatin in patients with advanced or recurrent ovarian cancer. Secord, A.A., Teoh, D.K., Barry, W.T., Yu, M., Broadwater, G., Havrilesky, L.J., Lee, P.S., Berchuck, A., Lancaster, J., Wenham, R.M. Clin. Cancer Res. (2012) [Pubmed]
  24. Cross-talk between EphA2 and BRaf/CRaf is a key determinant of response to Dasatinib. Huang, J., Hu, W., Bottsford-Miller, J., Liu, T., Han, H.D., Zand, B., Pradeep, S., Roh, J.W., Thanapprapasr, D., Dalton, H.J., Pecot, C.V., Rupaimoole, R., Lu, C., Fellman, B., Urbauer, D., Kang, Y., Jennings, N.B., Huang, L., Deavers, M.T., Broaddus, R., Coleman, R.L., Sood, A.K. Clin. Cancer Res. (2014) [Pubmed]
  25. Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model. Trevino, J.G., Summy, J.M., Lesslie, D.P., Parikh, N.U., Hong, D.S., Lee, F.Y., Donato, N.J., Abbruzzese, J.L., Baker, C.H., Gallick, G.E. Am. J. Pathol. (2006) [Pubmed]
  26. Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies. Schittenhelm, M.M., Shiraga, S., Schroeder, A., Corbin, A.S., Griffith, D., Lee, F.Y., Bokemeyer, C., Deininger, M.W., Druker, B.J., Heinrich, M.C. Cancer Res. (2006) [Pubmed]
  27. The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. Hantschel, O., Rix, U., Schmidt, U., Bürckstümmer, T., Kneidinger, M., Schütze, G., Colinge, J., Bennett, K.L., Ellmeier, W., Valent, P., Superti-Furga, G. Proc. Natl. Acad. Sci. U.S.A. (2007) [Pubmed]
  28. The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils. Kneidinger, M., Schmidt, U., Rix, U., Gleixner, K.V., Vales, A., Baumgartner, C., Lupinek, C., Weghofer, M., Bennett, K.L., Herrmann, H., Schebesta, A., Thomas, W.R., Vrtala, S., Valenta, R., Lee, F.Y., Ellmeier, W., Superti-Furga, G., Valent, P. Blood (2008) [Pubmed]
  29. Dasatinib cellular uptake and efflux in chronic myeloid leukemia cells: therapeutic implications. Hiwase, D.K., Saunders, V., Hewett, D., Frede, A., Zrim, S., Dang, P., Eadie, L., To, L.B., Melo, J., Kumar, S., Hughes, T.P., White, D.L. Clin. Cancer Res. (2008) [Pubmed]
  30. Brain accumulation of dasatinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by elacridar treatment. Lagas, J.S., van Waterschoot, R.A., van Tilburg, V.A., Hillebrand, M.J., Lankheet, N., Rosing, H., Beijnen, J.H., Schinkel, A.H. Clin. Cancer Res. (2009) [Pubmed]
  31. Activities of SYK and PLCgamma2 predict apoptotic response of CLL cells to SRC tyrosine kinase inhibitor dasatinib. Song, Z., Lu, P., Furman, R.R., Leonard, J.P., Martin, P., Tyrell, L., Lee, F.Y., Knowles, D.M., Coleman, M., Wang, Y.L. Clin. Cancer Res. (2010) [Pubmed]
WikiGenes - Universities