WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 201920
Description: MKC-1 is an orally bioavailable, small-molecule, bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking the formation of the mitotic spindle, which may result in cell cycle arrest at the G2/M phase and apoptosis. In addition, this agent has been shown to inhibit the activities of the oncogenic kinase Akt, the mTOR pathway, and importin-beta, a protein essential to the transport of other proteins from the cytosol into the nucleus. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). (Last updated:: 4/26/2016).
MedKoo Cat#: 201920
Chemical Formula: C22H16N4O4
Exact Mass: 400.11716
Molecular Weight: 400.39
Elemental Analysis: C, 66.00; H, 4.03; N, 13.99; O, 15.98
Synonym: MKC1; MKC 1; MKC-1; R 440; R-440; R440; Ro 317453; Ro-317453; Ro317453
IUPAC/Chemical Name: 3-(1-methyl-1H-indol-3-yl)-4-(1-methyl-6-nitro-1H-indol-3-yl)-1H-pyrrole-2,5-dione
InChi Key: OVSKGTONMLKNPZ-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H16N4O4/c1-24-10-15(13-5-3-4-6-17(13)24)19-20(22(28)23-21(19)27)16-11-25(2)18-9-12(26(29)30)7-8-14(16)18/h3-11H,1-2H3,(H,23,27,28)
SMILES Code: O=C(C(C1=CN(C)C2=C1C=CC=C2)=C3C4=CN(C)C5=C4C=CC([N+]([O-])=O)=C5)NC3=O
Phase 2 clinical trial results: 20 of an original target of 33 patients were accrued, with a median age of 61 (range 44-81). No objective responses were observed, with one patient demonstrating stable disease. Overall survival was 101 days from the start of MKC-1 administration, and median time to progression was 42 days. The most common adverse events listed as related or possibly related to MKC-1 administration were hematologic toxicities and fatigue. One patient developed grade 5 (fatal) pancytopenia. Grade 3 and 4 events included cytopenias (lymphopenia, anemia), hyperbilirubinemia, pneumonia, mucositis, fatigue, infusion reaction, anorexia, and hypoalbuminemia. CONCLUSIONS: MKC-1 administration was associated with substantial toxicity and did not demonstrate sufficient activity in patients with advanced pancreatic cancer to justify further exploration in this patient population. (source: Invest New Drugs. 2012 Aug;30(4):1614-20. ).
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