SM16
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- CAS号:
- 614749-78-9
- 英文名:
- SM16
- 英文别名:
- SM16;CS-2835;SM-16,TGF-β Receptor,Inhibitor,inhibit,SM 16,Transforming growth factor beta receptors,SM16;4-[4-(1,3-Benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]bicyclo[2.2.2]octane-1-carboxamide;Bicyclo[2.2.2]octane-1-carboxamide, 4-[4-(1,3-benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]-
- 中文名:
- SM16
- 中文别名:
- 化合物SM 16
- CBNumber:
- CB04656566
- 分子式:
- C25H26N4O3
- 分子量:
- 430.5
- MOL File:
- 614749-78-9.mol
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SM16化学性质
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沸点:
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691.3±55.0 °C(Predicted)
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密度:
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1.354±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO:65.0(Max Conc. mg/mL);150.99(Max Conc. mM)
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形态:
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A solid
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酸度系数(pKa):
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11.23±0.10(Predicted)
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SM16性质、用途与生产工艺
SM 16 是 ALK5/ALK4 激酶抑制剂，Ki 值分别为10 和 1.5 nM。
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.
SM16
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上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-111482 | SM 16 | | 1 mg | 500元 |
| 2024/04/30 | HY-111482 | SM16
SM 16 | 614749-78-9 | 5mg | 1100元 |
614749-78-9, SM16 相关搜索:
- 对照品
- 化合物SM 16
- 614749-78-9
- SM-16,TGF-β Receptor,Inhibitor,inhibit,SM 16,Transforming growth factor beta receptors,SM16
- SM16
- Bicyclo[2.2.2]octane-1-carboxamide, 4-[4-(1,3-benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]-
- CS-2835
- 4-[4-(1,3-Benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]bicyclo[2.2.2]octane-1-carboxamide