产品说明
一般描述
A cell-permeable, orally active, quinoxalinhydrazide derivative that acts an inhibitor of gp130. Binds to gp130 and induces its phosphorylation at Ser782 in ovarian cancer cells (OVCAR-8 and CaoV-3) in a time and dose-dependent manner. Shown to be cytotoxic in a number of ovarian cancer cell lines (IC50 = 720, 490, 950, 440, 530, 88-0, and 430 nM in OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY, and NCI/ADR-RES cells, respectively). Suppresses constitutive phosphorylation of and nuclear translocation of Stat3. Also blocks LIF and IL-6-induced Akt activation and phosphorylation of Stat3 (Y705) and Stat1 (Y701), without affecting their activation by IFN-γ. Reduces the level downstream effectors of gp130/Stat3 (survivin, MMP-7, Bcl-2, Bcl-xl, and cyclin D1) in ovarian cancer cells. Suppresses the growth of OVCAR-8 tumor xenografts in nude mice without affecting normal tissue (10 mg/kg, i.p. for 58 days).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell-permeable, orally active, quinoxalinhydrazide derivative that acts an inhibitor of gp130. Binds to gp130 and induces its phosphorylation at Ser782 in ovarian cancer cells (OVCAR-8 and CaoV-3) in a time and dose-dependent manner. Shown to be cytotoxic in a number of ovarian cancer cell lines (IC50 = 720, 490, 950, 440, 530, 88-0, and 430 nM in OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY, and NCI/ADR-RES cells, respectively). Suppresses constitutive phosphorylation of and nuclear translocation of Stat3. Also blocks LIF and IL-6-induced Akt activation and phosphorylation of Stat3 (Y705) and Stat1 (Y701), without affecting their activation by IFN-γ. Reduces the level downstream effectors of gp130/Stat3 (survivin, MMP-7, Bcl-2, Bcl-xl, and cyclin D1) in ovarian cancer cells. Suppresses the growth of OVCAR-8 tumor xenografts in nude mice without affecting normal tissue (10 mg/kg, i.p. for 58 days).
生化/生理作用
Primary Target
gp130
警告
Toxicity: Standard Handling (A)
其他说明
Xu, S., et al. 2013. Mol. Cancer Ther.12, 937.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C16H11FN6O · xHCl |
| 分子量 | 322.30 (free base basis) |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | light yellow |
| 溶解性 | DMSO: 100 mg/mL |
| 储存温度 | 2-8℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
