受注:045-509-1970 |
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Synonyms | CPI 1205, CPI1205 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C27H33F3N4O3 |
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分子量 | 518.57 | CAS No. | 1621862-70-1 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (192.83 mM) | |
Ethanol | 100 mg/mL (192.83 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 | Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2, with potential antineoplastic activity. |
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in vitro | Treatment with EZH2 inhibitor CPI-1205 cause apoptosis in multiple myeloma and plasmacytoma cell models[2]. |
in vivo | CPI-1205 shows excellent oral bioavailability. It was well-tolerated for repeat dosing as demonstrated by the absence of significant body weight loss. CPI-1205 shows relatively high clearance in both rats and dogs (3.19 L/h/kg and 1.41 L/h/kg, respectively) but demonstrates good oral bioavailability in both species(44.6% F in rats and 46.2% F in dogs). CPI-1205 was well-tolerated in the 28-day GLP toxicology studies, and any findings were reversible over the recovery period[1]. |
細胞アッセイ | 細胞株 | Cell-free assays |
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濃度 | 0.002 μM | |
反応時間 | ||
実験の流れ | ||
動物実験 | 動物モデル | CB-17 SCID mice |
投薬量 | 160 mg/kg orally twice daily | |
投与方法 | p.o |
ARID1A-deficient bladder cancer is dependent on PI3K signaling and sensitive to EZH2 and PI3K inhibitors [ JCI Insight, 2022, e155899] | PubMed: 35852858 |
Intrinsic immunogenicity of small cell lung carcinoma revealed by its cellular plasticity [ Cancer Discov, 2021, candisc.0913.2020] | PubMed: 33707236 |
Multi-omics analysis identifies therapeutic vulnerabilities in triple-negative breast cancer subtypes [ Nat Commun, 2021, 12(1):6276] | PubMed: 34725325 |
Druggable epigenetic suppression of interferon-induced chemokine expression linked to MYCN amplification in neuroblastoma [ J Immunother Cancer, 2021, 9(5)e001335] | PubMed: 34016720 |
EZH2 presents a therapeutic target for neuroendocrine tumors of the small intestine [ Sci Rep, 2021, 11(1):22733] | PubMed: 34815475 |
Multiple pharmacological inhibitors targeting the epigenetic suppressor enhancer of Zeste homolog 2 (EZH2) accelerate osteoblast differentiation [ Bone, 2021, S8756-3282(21)00155-1] | PubMed: 33940225 |
Precision Targeting with EZH2 and HDAC Inhibitors in Epigenetically Dysregulated Lymphomas [ Clin Cancer Res, 2019, 10.1158/1078-0432] | PubMed: 30979734 |
Precision Targeting with EZH2 and HDAC Inhibitors in Epigenetically Dysregulated Lymphomas [ Clin Cancer Res, 2019, 25(17):5271-5283] | PubMed: 30979734 |
Precision Targeting with EZH2 and HDAC Inhibitors in Epigenetically Dysregulated Lymphomas [ American Association for Cancer Research, 2019, 10.1158/1078-0432.CCR-18-3989] | PubMed: None |
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。