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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H24F5N5O |
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分子量 | 493.47 | CAS No. | 935273-79-3 | |
Solubility (25°C)* | 体外 | DMSO | 98 mg/mL (198.59 mM) | |
Ethanol | 98 mg/mL (198.59 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | MK-4101, a potent inhibitor of the Hedgehog pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells. |
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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[1]. |
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[1]. |
細胞アッセイ | 細胞株 | BCC(basal cell carcinoma) cells |
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濃度 | 10 μM | |
反応時間 | 72 h | |
実験の流れ | BCC cells are treated with MK-4101(10 μM) for 72 h and cell cycle is analyzed by FACS monitoring EdU incorporation. | |
動物実験 | 動物モデル | C57bl/6 mice or Sprague-Dawley rats. |
投薬量 | 40 or 80 mg/kg once a day; 80 mg/kg twice a day | |
投与方法 | oral administration |
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] | PubMed: 34997030 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。