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Chemical Compound Review

AC1NSJZZ     8-(2,6-dichlorophenyl)-3-[(4- fluoro-3...

Synonyms: CHEMBL574058, SureCN256711, CHEBI:47507, HKI-9924129, DNC000735, ...
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Disease relevance of PD180970


High impact information on PD180970


Anatomical context of PD180970

  • In this study, we show that blocking Bcr-Abl kinase activity using PD180970 in the human K562 CML cell line resulted in inhibition of Stat5 DNA-binding activity with an IC(50) of 5 nM [5].

Analytical, diagnostic and therapeutic context of PD180970


  1. Molecular characterization and sensitivity of STI-571 (imatinib mesylate, Gleevec)-resistant, Bcr-Abl-positive, human acute leukemia cells to SRC kinase inhibitor PD180970 and 17-allylamino-17-demethoxygeldanamycin. Nimmanapalli, R., O'Bryan, E., Huang, M., Bali, P., Burnette, P.K., Loughran, T., Tepperberg, J., Jove, R., Bhalla, K. Cancer Res. (2002) [Pubmed]
  2. Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571). La Rosée, P., Corbin, A.S., Stoffregen, E.P., Deininger, M.W., Druker, B.J. Cancer Res. (2002) [Pubmed]
  3. Activation of Stat3 by receptor tyrosine kinases and cytokines regulates survival in human non-small cell carcinoma cells. Song, L., Turkson, J., Karras, J.G., Jove, R., Haura, E.B. Oncogene (2003) [Pubmed]
  4. The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210Bcr-Abl tyrosine kinase and induces apoptosis of K562 leukemic cells. Dorsey, J.F., Jove, R., Kraker, A.J., Wu, J. Cancer Res. (2000) [Pubmed]
  5. Inhibition of Bcr-Abl kinase activity by PD180970 blocks constitutive activation of Stat5 and growth of CML cells. Huang, M., Dorsey, J.F., Epling-Burnette, P.K., Nimmanapalli, R., Landowski, T.H., Mora, L.B., Niu, G., Sinibaldi, D., Bai, F., Kraker, A., Yu, H., Moscinski, L., Wei, S., Djeu, J., Dalton, W.S., Bhalla, K., Loughran, T.P., Wu, J., Jove, R. Oncogene (2002) [Pubmed]
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