|Sabutoclax游离|CsnPharm

CAS No.: 1228108-65-3

Sabutoclax Catalog No. CSN19228

Synonyms: BI-97C1

Sabutoclax is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.

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技术信息

生物活性

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.4270 mL
- 7.1350 mL
- 14.2699 mL
- 5 mM
- 0.2854 mL
- 1.4270 mL
- 2.8540 mL
- 10 mM
- 0.1427 mL
- 0.7135 mL
- 1.4270 mL

技术信息

CAS号

1228108-65-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C42H40N2O8

运输

蓝冰

分子量

700.78

别名

BI-97C1

溶解度

DMSO	95.0 mg/mL (135.6 mM) warming
Water	Insoluble
Ethanol	26.0 mg/mL (37.1 mM) warming

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