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MK-4101

Cat. No. M8977
MK-4101 Structure
Size Price Availability Quantity
5mg USD 140 In stock
25mg USD 480 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

MK-4101 is a novel SMO antagonist of the Hedgehog Pathway. MK-4101 targets the Hh pathway in tumor cells, showing the maximum inhibitory effect on Gli1 MK-4101 also induced deregulation of cell cycle and block of DNA replication in tumors. 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.

MK-4101 was highly efficacious against primary medulloblastoma and BCC developing in the cerebellum and skin of Ptch1(+/-) mice. MK-4101 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.

Protocol
Cell Experiment
Cell lines BCC (basal cell carcinoma) cells
Preparation method BCC cells are treated with MK-4101(10 μM) for 72 h and cell cycle is analyzed by FACS monitoring EdU incorporation.
Concentrations 10 μM
Incubation time 72 h
Animal Experiment
Animal models C57bl/6 mice or Sprague-Dawley rats
Formulation 0.5% methylcellulose in deionized water
Dosages 40 or 80 mg/kg once a day; 80 mg/kg twice a day
Administration oral administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 493.47
Formula C24H24F5N5O
CAS Number 935273-79-3
Purity >98%
Solubility DMSO: ≥ 60 mg/mL
Storage at -20°C
References

MK-4101, a Potent Inhibitor of the Hedgehog Pathway, Is Highly Active against Medulloblastoma and Basal Cell Carcinoma.
Filocamo G, et al. Mol Cancer Ther. 2016 Jun;15(6):1177-89. PMID: 26960983.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MK-4101 supplier, Smo, inhibitors

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