[CAS NO. 935273-79-3] MK-4101
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PRODUCTS SPECIFICATIONS [935273-79-3]
Catalog
SLK-S8200
Brand
Selleck
CAS
935273-79-3
DESCRIPTION [935273-79-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 493.47 |
| Molecular Formula | C24H24F5N5O |
| SMILES | FC(C1=CC=CC=C1C2=NN=C(C34CCC(C5=NOC(C6CC(F)(F)C6)=N5)(CC4)CC3)N2C)(F)F |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0265 mL | 10.1323 mL | 20.2647 mL |
| 5 mM | 0.4053 mL | 2.0265 mL | 4.0529 mL |
| 10 mM | 0.2026 mL | 1.0132 mL | 2.0265 mL |
| 50 mM | 0.0405 mL | 0.2026 mL | 0.4053 mL |
Description
MK-4101, a potent inhibitor of the pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells.
Targets
| SMO [1] |
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 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.
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