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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 | C35H35FN6O3 |
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分子量 | 606.69 | CAS No. | 1242156-23-5 | ||||
Solubility (25°C)* | 体外 | DMSO (warmed with 50ºC water bath) | 62 mg/mL (102.19 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 | RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM. |
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in vitro | RN486 not only potently and selectively inhibits the Btk enzyme, but also displays functional activities in human cell-based assays in multiple cell types, blocking Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21.0 nM). RN486 is able to block the signaling of BCR as demonstrated by a marked inhibition of phosphorylation of both Btk and PLCγ2 in B cells. RN486 displays a selective B cell inhibitory profile in BioMAP Systems.[1] |
in vivo | RN486 displays similar functional activities in rodent models, effectively preventing type I and type III hypersensitivity responses. More importantly, RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibits both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood. [1] |
キナーゼアッセイ | Enzymatic Activity and Binding AssaysBtk Enzymatic Activity Assay. | |
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A fluorescence-based kinase assay is used to measure Btk kinase activity and its inhibition by RN486. In the assay, test compound is incubated with a human recombinant Btk (10 nM), ATP (100 μM), and a fluorescent-labeled peptide substrate (15 μM) at 30°C for 15 min. The reaction is then stopped by the addition of a termination buffer, and reaction product is quantified by using a Desktop Profiler 4 sipper. |
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。