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.
Sabutoclax 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
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
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