| CAS NO: | 935273-79-3 |
| 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 |
| Molecular Weight (MW) | 493.47 |
|---|---|
| Formula | C24H24F5N5O |
| CAS No. | 935273-79-3 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 98 mg/mL (198.59 mM) |
| Water: <1 mg/mL | |
| Ethanol: 60 mg/mL (121.58 mM) | |
| SMILES Code | FC(C1=CC=CC=C1C2=NN=C(C34CCC(C5=NOC(C6CC(F)(F)C6)=N5)(CC4)CC3)N2C)(F)F |
| Synonyms | MK-4101; MK 4101; MK4101 |
| In Vitro | In vitro activity: MK-4101 is a novel, potent and selective SMO inhibitor/antagonist of the Hedgehog (Hh) signaling pathway. MK-401 has the potential for the treatment of medulloblastoma and BCC (Basal Cell Carcinoma) as it is highly active against these cells. MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line (Gli Luc) with IC50 of 1.5 μM and in human KYSE180 oesophageal cancer cells with an IC50 of 1 μM. Furthermore, MK-4101 displaced a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 of 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 has displayed robust antitumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells. MK-4101 is highly efficacious against primary medulloblastoma and basal cell carcinoma(BCC) developing in the cerebellum and skin of Ptch1+/- mice. Pharmacokinetics of MK-4101 shows that it could be administered orally, showing a good bioavailability (F ≥ 87 %) with low-to-moderate plasma clearance in mice and rats. Moreover, it was well absorbed, and mainly excreted into the bile |
| Animal model | C57bl/6 mice or Sprague-Dawley rats. |
| Formulation & Dosage | 0.5% methylcellulose in deionized water. 40 or 80 mg/kg once a day; 80 mg/kg twice a day. oral administration |
| References | Mol Cancer Ther. 2016 Jun;15(6):1177-89. |
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