MKC-1

Names

[ Name ]:
MKC-1

[Synonym ]:
MKC-1
UNII-DNZ11VPY7Q
Bisindolylmaleimide deriv. 44
3-(1-methyl-3-indolyl)-4-(1-methyl-6-nitro-3-indolyl)-1H-pyrrole-2,5-dione
Ro-31-7453

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> mTOR

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> PI3K/Akt/mTOR >> Akt

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

[In Vivo]

MKC-1 (200 mg/kg, orally, daily) significantly increased the median survival time (MST) of mice bearing Caki-1 renal cell xenograft tumors[3].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₁₆N₄O₄

[ Molecular Weight ]:
400.38700

[ Exact Mass ]:
400.11700

[ PSA ]:
105.34000

[ LogP ]:
3.94450

Related Compounds

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