4-(4-氯-3-羟基苯基)-2-苯基-5-(吡啶-4-基)-1H-咪唑
| 中文名称 | 4-(4-氯-3-羟基苯基)-2-苯基-5-(吡啶-4-基)-1H-咪唑 |
|---|---|
| 中文同义词 | 4-(4-氯-3-羟基苯基)-2-苯基-5-(吡啶-4-基)-1H-咪唑;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;L-779450,RAF激酶抑制剂 |
| 英文名称 | 2-(Phenyl)-4-(3-hydroxy-4-chlorophenyl)-5-(4-pyridyl)-1H-imidazole |
| 英文同义词 | 2-(Phenyl)-4-(3-hydroxy-4-chlorophenyl)-5-(4-pyridyl)-1H-imidazole;L-779450;2-Chloro-5-[2-Phenyl-5-(4-pyridinyl)-1H-imidazol-4-yl]phenol;4-(4-Chloro-3-hydroxyphenyl)-2-phenyl-5-(4-pyridyl)-1H-iMidazole;Phenol, 2-chloro-5-[2-phenyl-4-(4-pyridinyl)-1H-iMidazol-5-yl]-;2-Chloro-5-(2-phenyl-5-(pyridin-4-yl)-1H-iMidazol-4-yl)phenol;2-chloro-5-[2-phenyl-4-(4-pyridinyl)-1H-imidazol-5-yl]phenol;4-(4-Chloro-3-hydroxyphenyl)-2-phenyl-5-(pyridin-4-yl)-1H-iMidazole |
| CAS号 | 303727-31-3 |
| 分子式 | C20H14ClN3O |
| 分子量 | 347.8 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;抑制剂;细胞生物学试剂;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 303727-31-3.mol |
| 结构式 |  |
4-(4-氯-3-羟基苯基)-2-苯基-5-(吡啶-4-基)-1H-咪唑 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(最大浓度 mg/mL);128.44(最大浓度 mM) DMF:30.0(最大浓度 mg/mL);86.26(最大浓度 mM) DMF:PBS ( pH 7.2) (1:7):0.12(最大浓度 mg/mL);0.35(最大浓度 mM) 乙醇:2.0(最大浓度 mg/mL);5.75(最大浓度 mM) |
| 形态 | 粉末 |
| 酸度系数(pKa) | 8.09±0.10(Predicted) |
| Target | Value |
|
B-Raf
(Cell-free assay) | 2.4 nM(Kd) |
|
B-Raf
(Cell-free assay) | 10 nM |
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.
安全信息
| 海关编码 | 2933399990 |
|---|
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-12787 | 4-(4-氯-3-羟基苯基)-2-苯基-5-(吡啶-4-基)-1H-咪唑 L-779450 | 303727-31-3 | 5mg | 650元 |
| 2024/01/25 | HY-12787 | 4-(4-氯-3-羟基苯基)-2-苯基-5-(吡啶-4-基)-1H-咪唑 L-779450 | 303727-31-3 | 10mM * 1mLin DMSO | 715元 |