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 | C35H34Cl2FN5O4S2 |
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分子量 | 742.71 | CAS No. | 1235034-55-5(free base) | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (134.64 mM) | |
Ethanol | 100 mg/mL (134.64 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 | A-1155463 Dihydrochloride, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM). |
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in vitro | A-1155463 Dihydrochloride disrupts BCL-XL-BIM but not BCL-2-BIM complexes in cells. A-1155463 kills BCL-XL-dependent Molt-4 cells (EC50=70 nM) but has no measurable cytotoxicity against BCL-2-dependent RS4;11 cells (EC50>5 mM). A-1155463 induces the hallmarks of apoptosis, as evidenced by the release of cytochrome c from mitochondria, caspase activation, and the accumulation of caspase-dependent sub-G0-G1 DNA content in BCL-XL-dependent H146 cells[2]. |
in vivo | Following a single 5 mg/kg IP dose of A-1155463 in nontumor bearing SCID-Beige mice, platelet counts fall dramatically as measured at 6 h postdose and then rebound to normal levels within 72 h. Daily Dosing at 5 mg/kg IP to SCID-Beige mice that had been inoculated with BCL-XL-dependent H146 tumor cells for 14 days causes a statistically significant inhibition of tumor growth (maximum tumor growth inhibition = 44%), which is alleviated upon cessation of dosing[1]. |
細胞アッセイ | 細胞株 | Colorectal cell lines (ATCC) |
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濃度 | 0-10 μM | |
反応時間 | 72 h | |
実験の流れ | Cells are treated with increasing concentration of A-1155463. Cells are assayed for viability after 72 h using the CellTiter-Glo luminescent cell viability assay according to the manufacturer’s protocol. Results are normalized to cells without treatment. EC50 is calculated using the GraphPad Prism software. |
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動物実験 | 動物モデル | SCID-Beige Mice |
投薬量 | 5 mg/kg | |
投与方法 | i.p. |
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Data from [Data independently produced by , , Oncogenesis, 2018, 7(9):74]
Clearance of defective muscle stem cells by senolytics restores myogenesis in myotonic dystrophy type 1 [ Nat Commun, 2023, 14(1):4033] | PubMed: 37468473 |
TRAF4-mediated ubiquitination-dependent activation of JNK/Bcl-xL drives radioresistance [ Cell Death Dis, 2023, 14(2):102] | PubMed: 36765039 |
Dual Targeting of Apoptotic and Signaling Pathways in T-Lineage Acute Lymphoblastic Leukemia [ Clin Cancer Res, 2023, 29(16):3151-3161] | PubMed: 37363966 |
Co-targeting BCL-XL and MCL-1 with DT2216 and AZD8055 synergistically inhibit small-cell lung cancer growth without causing on-target toxicities in mice [ Cell Death Discov, 2023, 9(1):1] | PubMed: 36588105 |
Co-targeting BCL-XL and MCL-1 with DT2216 and AZD8055 synergistically inhibit small-cell lung cancer growth without causing on-target toxicities in mice [ Cell Death Discov, 2023, 9(1):1] | PubMed: 36588105 |
The centrosomal protein 131 participates in the regulation of mitochondrial apoptosis [ Commun Biol, 2023, 6(1):1271] | PubMed: 38102401 |
Targeting Bcl-xL is a potential therapeutic strategy for extranodal NK/T cell lymphoma [ iScience, 2023, 26(8):107369] | PubMed: 37539026 |
Regulation of mitochondrial proteostasis by the proton gradient [ EMBO J, 2022, 41(16):e110476] | PubMed: 35912435 |
Cancer cell-intrinsic resistance to BiTE therapy is mediated by loss of CD58 costimulation and modulation of the extrinsic apoptotic pathway [ J Immunother Cancer, 2022, 10(3)e004348] | PubMed: 35296559 |
BCL6 inhibition ameliorates ruxolitinib resistance in CRLF2-rearranged acute lymphoblastic leukemia [ Haematologica, 2022, 10.3324/haematol.2022.280879] | PubMed: 36005560 |
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。