SR 11302 is an inhibitor of activator protein-1 (AP-1), a transcription factor that displays antitumor activity. SR 11302 does not activate transcription from the retinoic acid response element (RARE) and also does not display activity at retinoic acid receptors (EC50 > 1 μM for RARα, RARβ, and RARγ).
Inhibitor of activator protein-1 (AP-1) transcription factor activity that displays antitumor effects in vivo. Does not activate transcription from the retinoic acid response element (RARE) and displays no activity at retinoic acid receptors (EC50 > 1 μM for RARα, RARβ, RARγ and RXRα).
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Shiohara et al (1999) Effects of novel RAR- and RXR-selective retinoids on myeloid leukemic proliferation and differentiation in vitro. Blood 93 2057. PMID: 10068679.
[2] Huang et al (1997) Blocking activator protein-1 activity, but not activating retinoic acid response element, is required for the antitumor promotion effect of retinoic acid. Proc.Natl.Acad.Sci.USA 94 5826.
[3] Fanjul et al (1994) A new class of retinoids with selective inhibition of AP-1 inhibits proliferation. Nature 372 107. PMID:7969403.
分子式 C26H32O2 |
分子量 376.54 |
CAS号 160162-42-5 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mM |
Water <1 mg/mL |
Ethanol 10 mM |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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