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MK-4101

Chemical Structure : MK-4101

CAS No.: 935273-79-3

MK-4101 (MK 4101;MK4101)

Catalog No.: PC-42045Not For Human Use, Lab Use Only.

MK-4101 is a potent, orally bioavailable and brain penetrating Hedgehog pathway (Hh) inhibitor that inhibits Smoothened (Smo) with IC50 of 1.1 uM.

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Biological Activity

MK-4101 is a potent, orally bioavailable and brain penetrating Hedgehog pathway (Hh) inhibitor that inhibits Smoothened (Smo) with IC50 of 1.1 uM.
MK-4101 inhibits Hh signaling in a reporter gene assay in cancer cells with IC50 of 1-1.5 uM, also inhibited the proliferation of medulloblastoma cells derived from neonatally irradiated Ptch1−/+ mice in vitro with IC50 of 0.3 uM.
MK-4101 demonstrate a robust antitumor activity against Hh-driven tumors in vivo, shows potentiation for the treatment of medulloblastoma and BCC.

Physicochemical Properties

M.Wt 493.4723
Formula C24H24F5N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1,2,4-Oxadiazole, 5-(3,3-difluorocyclobutyl)-3-[4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]bicyclo[2.2.2]oct-1-yl]-

References

1. Filocamo G, et al. Mol Cancer Ther. 2016 Jun;15(6):1177-89.

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