| CAS NO: | 88349-90-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
Chemical Formula: C13H12ClNO3
Morlecular Weight: 265.69
| In Vitro | In vitro activity: MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line (Gli_Luc) with IC50 = 1.5 μM and in human KYSE180 oesophageal cancer cells with an IC50 = 1 μM. Furthermore, MK-4101 displaced a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 = 1.1 μM. MK-4101 arrests cells in G1 and G2 phases. Kinase Assay: MK-4101 is a novel, potent and selective SMO inhibitor/antagonist of the Hedgehog (Hh) signaling pathway. Cell Assay: BCC cells are treated with MK-4101(10 μM) for 72 h and cell cycle is analyzed by FACS monitoring EdU incorporation. |
|---|---|
| In Vivo | MK-4101 induce deregulation of cell cycle and block of DNA replication in tumors. MK-4101 targets the Hh pathway in tumor cells, showing the maximum inhibitory effect on Gli1. MK-4101 also induce deregulation of cell cycle and block of DNA replication in tumors. |
| Animal model | C57bl/6 mice or Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in 0.5% methylcellulose in deionized water; 40 or 80 mg/kg once a day; 80 mg/kg twice a day; Oral gavage |
| References | Mol Cancer Ther. 2016 Jun;15(6):1177-89. |
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