N-(吡啶-3-基)噻吩-2-羧酰胺
| 中文名称 | N-(吡啶-3-基)噻吩-2-羧酰胺 |
|---|---|
| 中文同义词 | N-(吡啶-3-基)噻吩-2-羧酰胺;化合物SW-106065 |
| 英文名称 | N-pyridin-3-ylthiophene-2-carboxamide |
| 英文同义词 | N-pyridin-3-ylthiophene-2-carboxamide;SW-106065;2-Thiophenecarboxamide, N-3-pyridinyl-;cell,SW 106065,cdk4,Inhibitor,MPNST,cycle,ATP,anticancer,cdk6,cyclin,SW106065,Apoptosis,inhibit |
| CAS号 | 62289-81-0 |
| 分子式 | C10H8N2OS |
| 分子量 | 204.25 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 62289-81-0.mol |
| 结构式 |  |
N-(吡啶-3-基)噻吩-2-羧酰胺 性质
| 沸点 | 270.8±15.0 °C(Predicted) |
|---|---|
| 密度 | 1.352±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：100 mg/mL（489.60 mM） |
| 酸度系数(pKa) | 12.39±0.70(Predicted) |
| 形态 | 固体 |
| 颜色 | 米白色至浅黄色 |
SW106065 (Compound 21, Cpd21) inhibits the human MPNST cell lines growth in a dose-dependent manner, and EC
50
concentrations of 439 nM and 753.6 nM for S462 and SNF96.2 cells, respectively. SW106065 remains nontoxic to normally dividing Schwann cells or mouse embryonic fibroblasts.
SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment shows a decreased percentage of cells in S phase, and a corresponding increased percentage in G1/G0 and G2/M.
SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment decreases the levels of cyclin A2, cyclin B1, cyclin D1, cyclin E, cdk4, and cdk6. And increases levels of cdkn1a and cdkn2a mRNA were observed in a dose-dependent manner.
SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment decreases the levels of Cyclin D1 protein.
SW106065 (Cpd21) treatment significant increase in the percentage of apoptotic cells.
Cell Cycle Analysis
| Cell Line: | sMPNST cells |
| Concentration: | 0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM |
| Incubation Time: | 24 hours |
| Result: | Showed a decreased percentage of cells in S phase, and a corresponding increased percentage in G1/G0 and G2/M. |
RT-PCR
| Cell Line: | sMPNST cells |
| Concentration: | 0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM |
| Incubation Time: | 24 hours |
| Result: | Decreased levels of cyclin A2, cyclin B1, cyclin D1, cyclin E, cdk4, and cdk6. Increased levels of cdkn1a and cdkn2a mRNA were observed in a dose-dependent manner. |
Western Blot Analysis
| Cell Line: | sMPNST cells |
| Concentration: | 0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM |
| Incubation Time: | 24 hours |
| Result: | Decreased levels of Cyclin D1 protein. |
SW106065 (Cpd21; 40 mg/kg; intraperitoneal injection; twice per day for 4 weeks) treatment can be delivered to mice in concentrations to sufficiently penetrate sMPNST tissue, and inhibit tumor development.
| Animal Model: | NCR-nu/nu female mice (6-7 week old) injected with MPNST cells |
| Dosage: | 40 mg/kg |
| Administration: | Intraperitoneal injection; twice per day for 4 weeks |
| Result: | Reduced MPNST burden in a mouse allograft model. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-124778 | SW106065 | 1 mg | 470元 | |
| 2024/04/30 | HY-124778 | N-(吡啶-3-基)噻吩-2-羧酰胺 SW106065 | 62289-81-0 | 5mg | 1180元 |