Evaluation of [11C]MPC-6827 as a microtubule targeting PET radiotracer in cancer lines

Evaluation of [11C]MPC-6827 in cancer

  • DILEEP KUMAR New York State Psychiatric Institute/ Columbia University https://orcid.org/0000-0001-6688-3991
  • Jaya Prabhakaran
  • Naresh Damuka
  • Justin W Hines
  • Steven J Kridel
  • J John Mann
  • Akiva Mintz
  • Kiran Kumar Solingapuram Sai


Microtubule (MTs) are implicated in the pathogenesis of cancer, and MT disruption with microtubule-targeted agents (MTA) is a valuable chemotherapeutic strategy. However, most MTAs developed to date are substrates for P-glycoprotein (p-GP) and multidrug resistance protein 1 (MDR1), preventing their use in the treatment of brain malignancies or as in vivo PET imaging agents in the brain.  [11C]MPC-6827 is the first brain-penetrating MTA based radiotracer, exhibits excellent uptake and specific binding in rodent brain. The objective of this study is to evaluate the uptake of [11C]MPC-6827 in cell lines of prostate, brain and breast malignancies. [11C]MPC-6827 provided the highest binding in breast cancer cell, MDA-MB-231, among all the cells studied, with 95% specific binding.  [11C]MPC-6827 binds to glioblastoma PDX and U251 cells with ~50% and 40% specific binding, whereas, prostate cancer cell line, PC3 cells showed 40% specific binding.  [11C]MPC-6827 also exhibits binding to the taxane and colchicine binding sites of MTs, in MDA-MB-231 cells. These data indicate that [11C]MPC-6827 can be a promising PET radiotracer for preclinical imaging of brain and peripheral cancers.

Keywords: PET, microtubule, radiotracer, cancer, cytoskeleton


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How to Cite
DILEEP KUMAR, J. Prabhakaran, N. Damuka, J. W. Hines, S. J. Kridel, J. J. Mann, A. Mintz, and K. K. Solingapuram Sai. “Evaluation of [11C]MPC-6827 As a Microtubule Targeting PET Radiotracer in Cancer Lines”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 12, no. 1, Nov. 2019, https://innovareacademics.in/journals/index.php/ijpps/article/view/35657.
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