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Sabutoclax

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Chemical Structure| 1228108-65-3 同义名 : BI-97C1
CAS号 : 1228108-65-3
货号 : A211104
分子式 : C42H40N2O8
纯度 : 98%
分子量 : 700.776
MDL号 : MFCD26142645
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(49.94 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Bcl-xL

    Bcl-xL, IC50:0.31 μM

  • Bfl-1

    Bfl-1, IC50:0.62 μM

  • Mcl-1

    Mcl-1, IC50:0.20 μM

  • Bcl-2

    Bcl-2, IC50:0.32 μM

    Bfl-1, IC50:0.62 μM
描述 Sabutoclax is a novel and effective pan-Bcl-2 antagonist with IC50 values of 0.31, 0.32, 0.20, and 0.62μM for inhibiting the binding of BH3 peptides to Bcl-XL, Bcl-2, Mcl-1, and Bfl-1. It potently inhibited cell growth of human prostate cancer PC-3, lung cancer H460, and lymphoma cell BP3 with EC50 values of 0.13, 0.56, and 0.049μM, respectively. Consistent with this in vitro study, Sabutoclax displayed antitumor efficacy in vivo as administration of Sabutoclax at 5mg/kg, i.p., every 2 days (total of nine injections), suppressed tumor growth of prostate cancer M2182 xenograft mouse model. Sabutoclax at 1μM significantly increased the apoptosis of BC LSCs measured by cleaved capase-3 and PI staining in vitro and sensitized marrow niche-engrafted BC LSCs to Dasatinib in vivo at 5mg/kg.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human H460 cells Cytotoxic assay 3 days Cytotoxicity against human H460 cells after 3 days by ATP-LITE assay, EC50=0.78 μM 20443627
human PC3 cells Cytotoxic assay 3 days Cytotoxicity against human PC3 cells after 3 days by ATP-LITE assay, EC50=4.64 μM 20443627
MEF 30 μM Function assay 24 h Induction of apoptosis in MEF expressing wild type Bcl-2 protein at 30 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based FACS analysis 20443627
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.43mL

0.29mL

0.14mL

7.13mL

1.43mL

0.71mL

14.27mL

2.85mL

1.43mL
参考文献

[1]Dash R, Azab B, et al. Apogossypol derivative BI-97C1 (Sabutoclax) targeting Mcl-1 sensitizes prostate cancer cells to mda-7/IL-24-mediated toxicity. Proc Natl Acad Sci U S A. 2011 May 24;108(21):8785-90.

[2]Wei J, Stebbins JL, et al. BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. J Med Chem. 2010 May 27;53(10):4166-76.