首页ApoptosisBCLObatoclax Mesylate
Obatoclax Mesylate
编号 T6275     别名: GX15-070, Obatoclax
CAS 803712-79-0     分子式 C20H19N3O·CH4O3S     分子量 413.49
靶点: Bcl-2;
Obatoclax is a Bcl-2 antagonist (Ki: 0.22 μM) and can induce apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3.
纯度:99.38%
规格 库存 单价 数量
2 mg 上海现货 584.00
5 mg 上海现货 869.00
10 mg 上海现货 1582.00
50 mg 上海现货 4907.00
100 mg 上海现货 8327.00
1 mL * 10 mM (in DMSO) 上海现货 869.00
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生物活性

产品描述

Obatoclax is a Bcl-2 antagonist (Ki: 0.22 μM) and can induce apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3.

靶点活性

Bcl-2,0.22μM(Ki)

实验溶液

30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL

体外活性

Obatoclax(5 μM)完全抑制SK-Mel5细胞中Mcl-1参与的Bak修复,并阻断由Mcl-1引起的抗ABT-373诱导的KB/Bcl-2细胞凋亡。Obatoclax对缺乏Bcl-xL或Bcl-xL低表达的细胞系有明显作用,而对所有强表达Mcl-1, Bcl-2,和Bcl-xL的细胞系的细胞毒性均较低。Obatoclax抑制多发性骨髓瘤细胞系如KMS12PE, KMS18, MY5等(IC50:52-1100nM)。Obatoclax可增强美法仑,地塞米松或硼替佐米的抗骨髓瘤活性。

体内活性

在携带人类C33A子宫瘤的SCID鼠中,Obatoclax(0.5 mg/kg)具有强抗癌活性。

激酶实验

Bcl-2 Binding affinity calculation: A predicted binding affinity for Obatoclax binding to BCL-2 is calculated using the SIE scoring function. [4] As a control in determining the reliability of the calculation, predicted binding affinities Ki) are calculated for a set of 12 small molecules with experimentally measured binding affinities to BCL-2.

细胞实验

Obatoclax is dissolved in DMSO at a stock concentration of 5 mM. Cell viability is assayed by MTT. Human MM cells (HMCLs), peripheral blood lymphocytes (PBLs), bone marrow stromal cells (BMSCs) are seeded in 96-well plates at a density of 2 × 104 per well for HMCLs or 5~10 × 103 for PBLs. Various concentrations of Obatoclax are added to the cells, with or without IGF-1 (50 ng/mL) or IL-6 (10 ng/mL). Cells are incubated for 48-72 hours and cell viability is determined.(Only for Reference)

细胞系: Human MM cells (HMCLs), peripheral blood lymphocytes (PBLs), bone marrow stromal cells (BMSCs)

动物实验

动物模型:FeBALB/c or CB17 SCID/SCID mice bearing SW480, C33A, PC3, and 4T1 cells are used.

化学信息

分子量

413.49

分子式

C20H19N3O·CH4O3S

CAS

803712-79-0

溶解度

DMSO: 77 mg/mL (186.2 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.418 ml 12.092 ml 24.184 ml
5 mM 0.484 ml 2.418 ml 4.837 ml
10 mM 0.242 ml 1.209 ml 2.418 ml
50 mM 0.048 ml 0.242 ml 0.484 ml
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