| Identification | Back Directory | [Name]
MKC-1 | [CAS]
125313-92-0 | [Synonyms]
MKC-1
Ro 31-7453
3-(1-Methylindol-3-yl)-4-(1-Methyl-6-nitroindol-3-yl)pyrrole-2,5-dione
3-(1-Methyl-1H-indol-3-yl)-4-(1-methyl-6-nitro-1H-indol-3-yl)-1H-pyrrole-2,5-dione
1H-Pyrrole-2,5-dione, 3-(1-methyl-1H-indol-3-yl)-4-(1-methyl-6-nitro-1H-indol-3-yl)-
inhibit,mTOR,Apoptosis,Protein kinase B,PKB,MKC 1,renal cell cancer,Caki-1,Mammalian target of Rapamycin,orally active,Microtubule/Tubulin,MKC-1,Akt,pancreatic cancer,Inhibitor,MKC1 | [Molecular Formula]
C22H16N4O4 | [MDL Number]
MFCD11983162 | [MOL File]
125313-92-0.mol | [Molecular Weight]
400.39 |
| Chemical Properties | Back Directory | [Melting point ]
173-174 °C | [Boiling point ]
714.5±60.0 °C(Predicted) | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
7.71±0.60(Predicted) | [color ]
Orange to red |
| Hazard Information | Back Directory | [Uses]
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]. | [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. DOI:10.1016/j.nucmedbio.2010.04.186
[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. DOI:10.1007/s10637-011-9708-3
[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. |
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