MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family[1][2][3].
MKC-1 (200 mg/kg, orally, daily) significantly increased the median survival time (MST) of mice bearing Caki-1 renal cell xenograft tumors[3].
[1]. Wang M, et al. The first design and synthesis of [11C]MKC-1 ([11C]Ro 31-7453), a new potential PET cancer imaging agent. Nucl Med Biol. 2010 Oct;37(7):763-75.
[2]. Faris JE, et al. A phase 2 study of oral MKC-1, an inhibitor of importin-β, tubulin, and the mTOR pathway in patients with unresectable or metastatic pancreatic cancer. Invest New Drugs. 2012 Aug;30(4):1614-20.
[3]. Burke P, et al. MKC-1 significantly increases survival of mice bearing renal cell carcinoma Caki-1 xenograft tumors through inhibition of the Akt/mTOR pathway[J]. Molecular Cancer Therapeutics, 2007(12):3524S-3525S.