MK-4101 是一种 SMO 拮抗剂 (对 293 细胞的 IC₅₀ 为 1.1 µM)，也是一种有效的 hedgehog 途径抑制剂 (对小鼠细胞的 IC₅₀ 为 1.5 µM；对 KYSE180 食管癌细胞的 IC₅₀ 为 1 µM)。MK-4101 具有强大的抗肿瘤活性，能抑制肿瘤细胞增殖并诱导细胞凋亡。

MK-4101 is a Smoothened (SMO) antagonist (IC 50 of 1.1 μM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC 50 of 1.5 μM for mouse cells; IC 50 of 1 μM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.

Solid

IC50: 1.1 μM (293 cells ); 1.5 μM (mouse cells); 1 μM (KYSE180 oesophageal cancer cells)

MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line with an IC50 of 1.5 μM, and in human KYSE180 oesophageal cancer cells with an IC50 of 1 μM. MK-4101 displaces a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 of 1.1 μM, implying that the compound binds to SMO. MK4101 also inhibits the proliferation of medulloblastoma cells derived from neonatallyirradiated Ptch1 mice in vitro with an IC50 of 0.3 μM.
MK-4101 (10 μM; 60 hours, 72 hours; medulloblastoma or BCC cells) treatment shows cell cycle arrest with a nearly complete disappearance of the S phase subpopulation, a prominent increase of the G1 population and, to a minor extent, of the G2 population.
MK-4101 (10 μM; medulloblastoma or BCC cells) tre

MK-4101 (40-80 mg/kg; oral administration; for 3.5 weeks; CD1 nude female mice) treatment shows tumor growth inhibition (40 and 80 mg/kg ) and tumor regression at the highest dose (80 mg/kg). MK-4101 treatment shows a dose-dependent down-regulation of Gli1 mRNA. The maximum effect for tumor inhibition and hedgehog pathway downregulation is achieved at 80 mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 50 mg/mL (101.32 mM)配制储备液