受注:045-509-1970 |
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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 | C21H21ClF2O4S |
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分子量 | 442.9 | CAS No. | 471905-41-6 | ||||
Solubility (25°C)* | 体外 | DMSO | 89 mg/mL (200.94 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. |
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in vitro | MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells. [1] In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation. [2] |
in vivo | MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16 , while decreases levels of Aβ 1-17. [1] In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain. [2] |
特徴 | A moderately potent γ-secretase inhibitor. |
動物実験 | 動物モデル | Cisterna Magna Ported (CMP) Rhesus Monkey Model. |
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投薬量 | ≤240 mg/kg | |
投与方法 | Administered via p.o. |
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Data from [Data independently produced by Oncotarget, 2014, 5(2), 363-74]
Data from [Data independently produced by , , Neoplasia, 2018, 21(1):93-105]
Data from [Data independently produced by , , Cancer Biol Ther, 2014, 15(5):633-42]
Distinct pathways drive anterior hypoblast specification in the implanting human embryo [ Nat Cell Biol, 2024, 26(3):353-365] | PubMed: 38443567 |
Simultaneous Inhibition of Ceramide Hydrolysis and Glycosylation Synergizes to Corrupt Mitochondrial Respiration and Signal Caspase Driven Cell Death in Drug-Resistant Acute Myeloid Leukemia [ Cancers (Basel), 2023, 15(6)1883] | PubMed: 36980769 |
In vitro antineoplastic effects of MK0752 in HPV-positive head and neck squamous cell carcinoma [ J Cancer Res Clin Oncol, 2023, 149(16):14691-14699] | PubMed: 37587308 |
Prediction of drug candidates for clear cell renal cell carcinoma using a systems biology-based drug repositioning approach [ EBioMedicine, 2022, 78:103963] | PubMed: 35339898 |
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] | PubMed: 34997030 |
Delta/Jagged-mediated Notch signaling induces the differentiation of agr2-positive epidermal mucous cells in zebrafish embryos [ PLoS Genet, 2021, 17(12):e1009969] | PubMed: 34962934 |
PLK1 and NOTCH Positively Correlate in Melanoma and their Combined Inhibition Results in Synergistic Modulations of Key Melanoma Pathways [ Mol Cancer Ther, 2020, molcanther.0654.2020] | PubMed: 33177155 |
A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] | PubMed: 31740922 |
DRUGPATH - a novel bioinformatic approach identifies DNA-damage pathway as a regulator of size maintenance in human ESCs and iPSCs [ Sci Rep, 2019, 9(1):1897] | PubMed: 30760778 |
IL6 blockade potentiates the anti-tumor effects of γ-secretase inhibitors in Notch3-expressing breast cancer. [ Cell Death Differ, 2018, 25(2):330-339] | PubMed: 29027990 |
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。