4-(4-氯-3-羟基苯基)-2-苯基-5-(吡啶-4-基)-1H-咪唑

4-(4-氯-3-羟基苯基)-2-苯基-5-(吡啶-4-基)-1H-咪唑化学性质

沸点 :579.8±50.0 °C(Predicted)
密度 :1.335±0.06 g/cm3(Predicted)
储存条件 :Sealed in dry,2-8°C
溶解度 :DMSO:44.67(Max Conc. mg/mL);128.44(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);86.26(Max Conc. mM)
DMF:PBS (pH 7.2) (1:7):0.12(Max Conc. mg/mL);0.35(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);5.75(Max Conc. mM)
形态 :Powder
酸度系数(pKa) :8.09±0.10(Predicted)
颜色 :Light yellow to yellow

安全信息

4-(4-氯-3-羟基苯基)-2-苯基-5-(吡啶-4-基)-1H-咪唑性质、用途与生产工艺

生物活性 L-779450是一种高效、低纳摩尔的B-raf抑制剂，IC50为10 nM，Kd为2.4 nM。
靶点
Target Value
B-Raf
(Cell-free assay) 2.4 nM(Kd)
B-Raf
(Cell-free assay) 10 nM
体外研究

L-779450 (L-779,450) shows a high degree of specificity towards Raf. The only other tested kinase inhibited is p38MAPK, which has a kinase domain structurally related to Raf. L-779450 inhibits anchorage-independent growth of human tumor lines at doses ranging from 0.3 to 2 μM. The effects of L-779450 (L-779,450) on TRAIL sensitivity are investigated here in melanoma cell lines with high TRAIL sensitivity (A-375 and SK-Mel-147), moderate sensitivity (Mel-HO, SK-Mel-13, and SK-Mel-28), and permanent resistance (MeWo, Mel-2a, and SK-Mel-103), as well as in TRAIL-selected cell lines with acquired resistance (A-375-TS and Mel-HO-TS). Despite only moderate direct effects of L-779450 on apoptosis, it strongly enhances TRAIL-induced apoptosis in sensitive melanoma cells and overrules TRAIL resistance in Mel-2a, SK-Mel-103, A-375-TS, and Mel-HO-TS. At 24 hours, 16-35% apoptosis induction is obtained.

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