Powder: -20°C for 3 years | In solvent: -80°C for 1 year
UMI-77是一种选择性的Mcl-1抑制剂,结合到Mcl-1的 BH3 结合沟,Ki 值为 490 nM,对 Bcl-2 家族的其他成员具有选择性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 313 | 现货 | ||
2 mg | ¥ 463 | 现货 | ||
5 mg | ¥ 788 | 现货 | ||
10 mg | ¥ 1,190 | 现货 | ||
25 mg | ¥ 2,170 | 现货 | ||
50 mg | ¥ 3,620 | 现货 | ||
100 mg | ¥ 4,570 | 现货 | ||
200 mg | ¥ 7,380 | 现货 | ||
500 mg | ¥ 10,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 855 | 现货 |
产品描述 | UMI-77, a specific Mcl-1 inhibitor (Ki: 490 nM), has selectivity over other members of Bcl-2 family. |
靶点活性 | MCL-1:490 nM(Ki) |
体外活性 | UMI-77(60 mg/kg, i.v. )在BxPC-3异种移植小鼠模型中具有单剂量抗肿瘤活性且不损害正常组织 |
体内活性 | UMI-77可激活固有的凋亡通路和/或Bax构象改变,从而促使胰腺癌细胞凋亡。UMI-77可干扰细胞 Mcl-1和BL-Noxa间的相互作用,还干扰Mcl-1/Bax蛋白-蛋白相互作用。UMI-77抑制胰腺癌细胞的生长,如BxPC-3,Panc-1,MiaPaCa-2,AsPC-1 和 Capan-2细胞(IC50:3.4/4.4/12.5/16.1/5.5 μM)。 |
激酶实验 | Fluorescence polarization (FP)-based binding assays: Based on the Kd values, the concentrations of the proteins used in the competitive binding experiments are 90 nM for Mcl-1, 40 nM for Bcl-w, 50 nM for Bcl-xL, 60 nM for Bcl-2, and 4 nM for A1/Bfl-1. The fluorescent probes, Flu-BID and FAM-BID are fixed at 2 nM for all assays except for A1/Bfl-1 where FAMBID is used at 1 nM. 5 μL of the tested compound in DMSO and 120 μL of protein/probe complex in the assay buffer (100 mM potassium phosphate, pH 7.5; 100 μg/ml bovine gamma globulin; 0.02% sodium azide) are added to assay plates (Microfluor 2Black), incubated at room temperature for 3 h and the polarization values (mP) are measured at an excitation wavelength at 485 nm and an emission wavelength at 530 nm using the plate reader Synergy H1Hybrid. IC50 values are determined by nonlinear regression fitting of the competition curves. |
细胞实验 | Human pancreatic cancer cell lines AsPC-1, BxPC-3, and Capan-2 are cultured in RPMI-1640 medium, whereas Panc-1 and MiaPaCa are cultured in Dulbeccos' Modified Eagle's Medium (DMEM), all supplemented with 10% FBS. The cell growth inhibition after treatment with increasing concentrations of the compounds is determined by WST-8 assay.(Only for Reference) |
别名 | UMI77, UMI 77 |
分子量 | 468.34 |
分子式 | C18H14BrNO5S2 |
CAS No. | 518303-20-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 86 mg/mL (183.6 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 86 mg/mL (183.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.1352 mL | 10.676 mL | 21.352 mL | 53.38 mL |
5 mM | 0.427 mL | 2.1352 mL | 4.2704 mL | 10.676 mL | |
10 mM | 0.2135 mL | 1.0676 mL | 2.1352 mL | 5.338 mL | |
20 mM | 0.1068 mL | 0.5338 mL | 1.0676 mL | 2.669 mL | |
50 mM | 0.0427 mL | 0.2135 mL | 0.427 mL | 1.0676 mL | |
100 mM | 0.0214 mL | 0.1068 mL | 0.2135 mL | 0.5338 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。
UMI-77 518303-20-3 Apoptosis BCL Bcl-2 Family Inhibitor UMI77 UMI 77 inhibit inhibitor