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.
Product information
CAS Number: 125313-92-0
Molecular Weight: 400.39
Formula: C22H16N4O4
Chemical Name: 3-(1-methyl-1H-indol-3-yl)-4-(1-methyl-6-nitro-1H-indol-3-yl)-1H-pyrrole-2, 5-dione
Smiles: CN1C=C(C2=C(C3=CN(C)C4=CC=CC=C34)C(=O)NC2=O)C2=CC=C(C=C12)[N+]([O-])=O
InChiKey: OVSKGTONMLKNPZ-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
References:
- Zagouri F, Sergentanis TN, Chrysikos D, Filipits M, Bartsch R. mTOR inhibitors in breast cancer: A systematic review. Gynecol Oncol. 2012 Dec;127(3):662-72. doi: 10.1016/j.ygyno.2012.08.040. Epub 2012 Sep 9. PubMed PMID: 22967800.
- Faris JE, Arnott J, Zheng H, Ryan DP, Abrams TA, Blaszkowsky LS, Clark JW, Enzinger PC, Hezel AF, Ng K, Wolpin BM, Kwak EL. 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. doi: 10.1007/s10637-011-9708-3. Epub 2011 Jul 29. PubMed PMID: 21800081.
- Tevaarwerk A, Wilding G, Eickhoff J, Chappell R, Sidor C, Arnott J, Bailey H, Schelman W, Liu G. Phase I study of continuous MKC-1 in patients with advanced or metastatic solid malignancies using the modified Time-to-Event Continual Reassessment Method (TITE-CRM) dose escalation design. Invest New Drugs. 2012 Jun;30(3):1039-45. Epub 2011 Jan 12. PubMed PMID: 21225315; PubMed Central PMCID: PMC3139017.
Products are for research use only. Not for human use.
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