中文名 | L-779450 |
英文名 | L-779450 |
别名 | RAF激酶抑制剂(L-779450) 2-氯-5-(2-苯基-5-(吡啶-4-基)-1H-咪唑-4-基)苯酚 2-氯-5-(2-苯基-5-(吡啶-4-基)-1H-咪唑-5-基)苯酚 4-(4-氯-3-羟基苯基)-2-苯基-5-(吡啶-4-基)-1H-咪唑 |
英文别名 | L-779450 2-Chloro-5-[2-Phenyl-5-(4-pyridinyl)-1H-imidazol-4-yl]phenol 2-chloro-5-[2-phenyl-4-(4-pyridinyl)-1H-imidazol-5-yl]phenol 2-Chloro-5-(2-phenyl-5-(pyridin-4-yl)-1H-iMidazol-4-yl)phenol Phenol, 2-chloro-5-[2-phenyl-4-(4-pyridinyl)-1H-iMidazol-5-yl]- 4-(4-Chloro-3-hydroxyphenyl)-2-phenyl-5-(4-pyridyl)-1H-iMidazole 2-(Phenyl)-4-(3-hydroxy-4-chlorophenyl)-5-(4-pyridyl)-1H-imidazole 4-(4-Chloro-3-hydroxyphenyl)-2-phenyl-5-(pyridin-4-yl)-1H-iMidazole |
CAS | 303727-31-3 |
化学式 | C20H14ClN3O |
分子量 | 347.8 |
密度 | 1.335±0.06 g/cm3(Predicted) |
沸点 | 579.8±50.0 °C(Predicted) |
酸度系数 | 8.09±0.10(Predicted) |
存储条件 | Sealed in dry,2-8°C |
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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.875 ml | 14.376 ml | 28.752 ml |
5 mM | 0.575 ml | 2.875 ml | 5.75 ml |
10 mM | 0.288 ml | 1.438 ml | 2.875 ml |
5 mM | 0.058 ml | 0.288 ml | 0.575 ml |
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