935273-79-3 Usage
Biological Activity
mk-4101 is a hedgehog (hh) signaling pathway inhibitor.abnormal activation of the hedgehog (hh) signaling pathway is reported in the pathogenesis of various cancers, such as medulloblastoma and basal cell carcinoma.
in vitro
mk-4101 was found to target the hh pathway in tumor cells, with the maximum inhibitory effect on gli1. mk-4101 could also induce the deregulation of cell cycle and block of dna replication in tumors. in addition, members of the igf and wnt signaling pathways were among the most highly deregulated genes by mk-4101, indicating that the interplay among hh, igf, and wnt was critical in hh-dependent tumorigenesis [1].
in vivo
in a previous study, using neonatally irradiated ptch1(+/-) mice as a model of hh-dependent tumors, the in vivo effects of mk-4101 was investigated for the treatment of medulloblastoma and basal cell carcinoma. results showed a potent antitumor activity of mk-4101, achieved by the inhibition of proliferation and induction of extensive apoptosis. moreover, beside antitumor activity on transplanted tumors, mk-4101 was found to be highly efficacious against primary medulloblastoma and basal cell carcinoma in the cerebellum and skin [1].
IC 50
1.5 μmol/l for in mouse light ii cells by gli_luc assay
references
[1] filocamo g et al. mk-4101, a potent inhibitor of the hedgehog pathway, is highly active against medulloblastoma and basal cell carcinoma. mol cancer ther. 2016 jun;15(6):1177-89.
Check Digit Verification of cas no
The CAS Registry Mumber 935273-79-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,3,5,2,7 and 3 respectively; the second part has 2 digits, 7 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 935273-79:
(8*9)+(7*3)+(6*5)+(5*2)+(4*7)+(3*3)+(2*7)+(1*9)=193
193 % 10 = 3
So 935273-79-3 is a valid CAS Registry Number.
935273-79-3Relevant articles and documents
Triazole derivatives which are SMO antagonists
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Page/Page column 12; 13, (2008/12/04)
The present invention provides a method for the treatment or prevention of conditions which can be ameliorated by Smo antagonism, which method comprises administration to a patient in need thereof of an effective amount of a compound of formula I or a com
