SM16
| 中文名称 | SM16 |
|---|---|
| 中文同义词 | 化合物SM 16;4-(4-(苯并[D][1,3]二氧杂环戊烯-5-基)-5-(6-甲基吡啶-2-基)-1H-咪唑-2-基)二环[2.2.2]辛烷-1-甲酰胺;化合物SM 16,10 MM DMSO 溶液;SM 16 |CAS 614749-78-9 |
| 英文名称 | SM16 |
| 英文同义词 | 4-[4-(1,3-Benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]bicyclo[2.2.2]octane-1-carboxamide;CS-2835;Bicyclo[2.2.2]octane-1-carboxamide, 4-[4-(1,3-benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]-;SM16;SM-16,TGF-β Receptor,Inhibitor,inhibit,SM 16,Transforming growth factor beta receptors,SM16;4-[5-(2H-1,3-benzodioxol-5-yl)-4-(6-methylpyridin-2-yl)-1H-imidazol-2-yl]bicyclo[2.2.2]octane-1-carboxamide;SM 16, 10 mM in DMSO |
| CAS号 | 614749-78-9 |
| 分子式 | C25H26N4O3 |
| 分子量 | 430.5 |
| EINECS号 | |
| 相关类别 | 对照品 |
| Mol文件 | 614749-78-9.mol |
| 结构式 |  |
SM16 性质
| 沸点 | 691.3±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.354±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO:65.0(最大浓度 mg/mL);150.99(最大浓度 mM) |
| 形态 | 固体 |
| 酸度系数(pKa) | 11.23±0.10(Predicted) |
| 颜色 | 白色至米白色 |
Ki: ALK5 (10 nM), ALK4 (1.5 nM)
SM 16 inhibits TGFβ-induced plasminogen activator inhibitor-luciferase activity (IC 50 =64 nM) and TGFβ- or activin-induced Smad2 phosphorylation at concentrations between 100 and 620 nM. SM 16 is tested against >60 related and unrelated kinases and shows moderate off-target activity only against Raf (IC 50 =1 μM) and p38/SAPKa (IC 50 =0.8 μM). SM 16 exhibits no inhibitory activity against ALK family members ALK1 and ALK6.
SM 16 penetrates tumor cells in vivo , suppressing tumor phosphorylated Smad2/3 levels for at least 3 h following treatment of tumor-bearing mice with a single i.p. bolus of 20 mg/kg SM 16. The growth of established AB12 tumors is significantly inhibited by 5 mg/kg/d SM 16 (P<0.001) delivered via s.c. miniosmotic pumps over 28 days.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/09/15 | HY-111482 | SM 16 | 614749-78-9 | 1 mg | 500元 |
| 2026/09/15 | HY-111482 | SM16 SM 16 | 614749-78-9 | 5mg | 1100元 |