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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 | C20H18N6O3.2HCl |
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分子量 | 463.32 | CAS No. | 648903-57-5 | ||||
Solubility (25°C)* | 体外 | DMSO | 6 mg/mL (12.95 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 | BAY-61-3606 is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM). BAY-61-3606 induces cell cycle arrest and apoptosis. |
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in vitro | BAY 61-3606 is a highly selective inhibitor of Syk kinase. Other selected tyrosine kinases, Lyn, Fyn, Src, Itk, and Btk, are not inhibited by BAY 61-3606 in concentrations up to 4.7 μM. BAY 61-3606 is also found to inhibit B cell receptor (BCR)-mediated signaling[1]. Bay 61-3606 is a sensitizer of TRAIL-induced apoptosis. Mcl-1 downregulation by Bay 61-3606 are concentration- and time-dependent in MCF-7 cells. phosphorylation of Syk is reduced by Bay 61-3606 in MCF-7 and T47D cells. Downregulation of Mcl-1 by Bay 61-3606 is independent of Syk in breast cancer cells. Bay 61-3606 promotes the ubiquitin/proteasome-dependent degradation of the Mcl-1 protein in MCF-7 cells. Bay 61-3606 inhibits the phosphorylation of CDK9, RNA polymerase II, and Mcl-1 expression in MCF-7 cells. Bay 61-3606 inhibits CDK9 kinase activity with an in vitro IC50 of 37 nM[2]. |
in vivo | After 20 days of drug administration, the volume of the xenografted tumor was significantly (P <0.001) reduced the efficacy of Bay 61–3606 when administered in TRAIL combination[2]. Oral administration of BAY 61-3606 to rats significantly suppresses antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuates antigen-induced airway inflammation in rats[1]. |
細胞アッセイ | 細胞株 | MCF-7 cells |
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濃度 | 2.5 μM or 5 μM | |
反応時間 | 12 h or 24 h | |
実験の流れ | MCF-7 cells are exposed to TRAIL (indicated concentrations:0, 12.5, 25, 37.5 ng/ml) with or without Bay 61-3606 (2.5 μM) for 24 h; After exposure to the agents for 12 h, MCF-7 cells are subjected to immunocytochemistry using an active Bak antibody; Caspase activity is measured in MCF-7 cells exposed to Bay 61-3606 (5 μM) with or without TRAIL (50 ng/ml) for 24 h. |
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動物実験 | 動物モデル | xenograft-bearing BALB/c nude mice |
投薬量 | 50 mg/kg | |
投与方法 | i.p. |
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Probucol protects against brain damage caused by intra-neural pyroptosis in rats with vascular dementia through inhibition of the Syk/Ros pathway [ Aging (Albany NY), 2024, 16(5):4363-4377] | PubMed: 38441564 |
HP1 induces ferroptosis of renal tubular epithelial cells through NRF2 pathway in diabetic nephropathy [ Open Life Sci, 2023, 18(1):20220678] | PubMed: 37589000 |
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226] | PubMed: 36266272 |
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226] | PubMed: 36266272 |
ARPC1B binds WASP to control actin polymerization and curtail tonic signaling in B cells [ JCI Insight, 2021, e149376] | PubMed: 34673575 |
Dectin-2-mediated initiation of immune responses caused by influenza virus hemagglutinin [ Biomed Res, 2021, 42(2):53-66] | PubMed: 33840686 |
Mapping phospho-catalytic dependencies of therapy-resistant tumours reveals actionable vulnerabilities. [ Nat Cell Biol, 2019, 21(6):778-790] | PubMed: 31160710 |
Berberine suppresses mast cell-mediated allergic responses via regulating FcɛRI-mediated and MAPK signaling. [ Int Immunopharmacol, 2019, 71:1-6] | PubMed: 30861392 |
Multiple sources of signal amplification within the B-cell Ras/MAPK pathway. [ Mol Biol Cell, 2019, 30(13):1610-1620] | PubMed: 31042097 |
Phosphorylation-Mediated IFN-γR2 Membrane Translocation Is Required to Activate Macrophage Innate Response [Xu X, et al. Cell, 2018, 175(5):1336-1351] | PubMed: 30318148 |
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。