store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sabutoclax (BI-97C1) 是一种泛 Bcl-2 抑制剂,包括 Bcl-xL、Bcl-2、Mcl-1 和 Bfl-1,IC50 分别为 0.31 μM、0.32 μM、0.20 μM 和 0.62 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 575 | 现货 | ||
5 mg | ¥ 1,390 | 现货 | ||
10 mg | ¥ 2,230 | 现货 | ||
25 mg | ¥ 4,490 | 现货 | ||
50 mg | ¥ 6,570 | 现货 | ||
100 mg | ¥ 8,860 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,550 | 现货 |
产品描述 | Sabutoclax (BI-97C1)(BI-97C1) 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. |
靶点活性 | Bcl-xL:0.31 μM, Bfl-1:0.62 μM, BCL2:0.32 μM, Mcl-1:0.2 μM |
体外活性 |
Sabutoclax (0.001-10 μM; 72 hours) inhibits the growth of human prostate cancer and lung cancer cell lines[2]. Sabutoclax (0.01-1 μM; 24-48 hours) induces apoptosis in human diffuse large B-cell lymphoma cells[2]. Sabutoclax (0-15 μM; 48 hours) upregulates the levels of pro-apoptotic proteins in chemotherapy-resistant cells[1]. |
体内活性 | Sabutoclax (1-5 mg/kg; intraperitoneal injection; every two days for a total of 18 days) reduces the growth of M2182 tumors in nude mice[2]. |
激酶实验 | Competitive fluorescence polarization assays (FPA) : A Bak BH3 peptide (F-BakBH3) (GQVGRQLAIIGDDINR) is labeled at the N-terminus with fluorescein isothiocyanate (FITC) and purified by HPLC. For competitive binding assays, 100 nM GST-Bcl-XL ΔTM protein is preincubated with the tested compound at varying concentrations in 47.5 μL PBS (pH = 7.4) in 96-well black plates at room temperature for 10 min, and then 2.5 μL of 100 nM FITC-labeled Bak BH3 peptide is added to produce a final volume of 50 μL. The wild-type and mutant Bak BH3 peptides are included in each assay plate as positive and negative controls, respectively. After 30 min incubation at room temperature, the polarization values in millipolarization units are measured at excitation/emission wavelengths of 480/535 nm with a multilabel plate reader. IC50 is determined by fitting the experimental data to a sigmoidal dose-response nonlinear regression model. Data reported are mean of three independent experiments. Performance of Bcl-2 and Mcl-1FPA are similar. Briefly, 50 nM of GST-Bcl-2 or -Mcl-1are incubatedwith various concentrations of compound (4 and 11-14) for 2 min, and then 15 nM FITC-conjugated-Bim BH3 peptide is added in PBS buffer. Fluorescence polarization is measured after 10 min. |
细胞实验 | ATP-LITE assay(Only for Reference) |
别名 | BI-97C1 |
分子量 | 700.78 |
分子式 | C42H40N2O8 |
CAS No. | 1228108-65-3 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 22 mg/mL(31.4 mM)
DMSO: 93 mg/mL (132.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.427 mL | 7.1349 mL | 14.2698 mL | 35.6745 mL |
5 mM | 0.2854 mL | 1.427 mL | 2.854 mL | 7.1349 mL | |
10 mM | 0.1427 mL | 0.7135 mL | 1.427 mL | 3.5675 mL | |
20 mM | 0.0713 mL | 0.3567 mL | 0.7135 mL | 1.7837 mL | |
DMSO | 50 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.7135 mL |
100 mM | 0.0143 mL | 0.0713 mL | 0.1427 mL | 0.3567 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Sabutoclax 1228108-65-3 Apoptosis BCL BI-97C1 Inhibitor inhibitor inhibit