Information MK-4101, a potent inhibitor of theHedgehogpathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells. Targets SMO In vitro 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. In vivo MK-4101 has robust antitumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells. MK-4101 is highly efficacious against primary medulloblastomaand 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. Cell Research(from reference) Cell lines：BCC(basal cell carcinoma) cells Concentrations：10 μM Incubation Time：72 h
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MK-4101
CAS number：935273-79-3 molecular formula：C24H24F5N5O
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| Chinese alias | - | ||
| English alias | 5-(3,3-difluorocyclobutyl)-3-(4-(4-methyl-5-(2-(trifluoromethyl)phenyl)-4H-1,2,4-triazol-3-yl)bicyclo[2.2.2]octan-1-yl)-1,2,4-oxadiazole | ||
| CAS number | 935273-79-3 | molecular formula | C24H24F5N5O |
| molecular weight | 493.47 g/mol | Exact mass | 10mM in DMSO |
| PSA | 69.600 Ų | logp | 4.784 |
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