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Synonyms | S 055746,BCL201 | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C43H42N4O6 |
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分子量 | 710.82 | CAS No. | 1448584-12-0 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (140.68 mM) | |
Water | Insoluble | |||
Ethanol | 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 | S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds. |
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in vitro | S55746 occupies the hydrophobic groove of BCL-2. In a panel of hematological cell lines, S55746 induces hallmarks of apoptosis including externalization of phosphatidylserine, caspase-3 activation and PARP cleavage. S55746 potently induces RS4;11 cell killing after 72 h of treatment with an IC50 of 71.6 nM and exhibits a much weaker activity in H146 (IC50 = 1.7 μM), a BCL-XL-dependent cell line, which expresses a low level of BCL-2 and high level of BCL-XL. It has no cytotoxic activity on BCL-XL-dependent cells, such as platelets[1]. |
in vivo | S55746 administered by oral route daily in mice demonstrates robust anti-tumor efficacy in two hematological xenograft models (RS4;11 and Toledo models) with no weight lost and no change in behavior[1]. |
細胞アッセイ | 細胞株 | RS4;11 cells |
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濃度 | 0.01, 0.03, 0.1, 0.3, 1 μM | |
反応時間 | 2 hours | |
実験の流れ | Apoptosis induction in RS4;11 cells treated with S55746 at various concentrations for 2 h. Cells were analyzed by flow cytometry for PI and annexin V-FITC labeling. |
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動物実験 | 動物モデル | RS4;11 tumor xenografts (Female SCID mice inoculated with RS4;11 cells) |
投薬量 | 25 and 100 mg/kg | |
投与方法 | p.o. |
Obatoclax Rescues FUS-ALS Phenotypes in iPSC-Derived Neurons by Inducing Autophagy [ Cells, 2023, 12(18)2247] | PubMed: 37759469 |
Obatoclax Rescues FUS-ALS Phenotypes in iPSC-Derived Neurons by Inducing Autophagy [ Cells, 2023, 10.3390/cells12182247] | PubMed: 37759469 |
Activation of RAS/MAPK pathway confers MCL-1 mediated acquired resistance to BCL-2 inhibitor venetoclax in acute myeloid leukemia [ Signal Transduct Target Ther, 2022, 7(1):51] | PubMed: 35185150 |
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。