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TitleBI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis.
Journal, issue, pagesMol. Cancer Ther., Vol. 14, Page 2762-2772, Year 2015
Publish dateSep 30, 2015 (structure data deposition date)
AuthorsSanderson, M.P. / Apgar, J. / Garin-Chesa, P. / Hofmann, M.H. / Kessler, D. / Quant, J. / Savchenko, A. / Schaaf, O. / Treu, M. / Tye, H. ...Sanderson, M.P. / Apgar, J. / Garin-Chesa, P. / Hofmann, M.H. / Kessler, D. / Quant, J. / Savchenko, A. / Schaaf, O. / Treu, M. / Tye, H. / Zahn, S.K. / Zoephel, A. / Haaksma, E. / Adolf, G.R. / Kraut, N.
External linksMol. Cancer Ther. / PubMed:26438154
MethodsX-ray diffraction
Resolution2.264 Å
Structure data

PDB-5e1s:
The Crystal structure of INSR Tyrosine Kinase in complex with the Inhibitor BI 885578
Method: X-RAY DIFFRACTION / Resolution: 2.264 Å

Chemicals

ChemComp-5JA:
(5R)-N-(1-{2-[4-(2-methoxyethyl)piperazin-1-yl]ethyl}-1H-pyrazol-3-yl)-5,8-dimethyl-9-phenyl-6,8-dihydro-5H-pyrazolo[3,4-h]quinazolin-2-amine

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / Kinase / INSR / IGF-1R / Inhibitor

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