产品说明书
PLX4720
 |
同义名 : | - |
| CAS号 : | 918505-84-7 | |
| 货号 : | A332013 | |
| 分子式 : | C17H14ClF2N3O3S | |
| 纯度 : | 99+% | |
| 分子量 : | 413.826 | |
| MDL号 : | MFCD14635203 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 105 mg/mL(253.73 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
2% DMSO+50% PEG 300+5% Tween 80+water 5 mg/mL |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
|
||
| 描述 | The RAS/RAF signaling pathway is an important mediator of tumor cell proliferation and angiogenesis. PLX4720 is a potent and selective inhibitor of B-RafV600E mutant, with less potent to wt-braf and BRK with IC50 values of 160nM and 130nM, and showed selectivity to B-RafV600E mutant over 100 fold against a diverse panel of 70 other kinases. Consistent with the in vitro study, PLX4720 showed more potent anti-proliferation in tumor cell lines bearing the B-RafV600E oncogene with GI50<1.7μM,such as COLO205, A375, WM2664 and COLO829 cells, versus GI50>10μM on cells with wt-braf. PLX4720 initiates antimelanoma activity, inhibition of MAPK pathway represented suppressed p-ERK, apoptotic response only in cells harboring the V600E mutation. Daily oral gavage of PLX4720, at dose of 20mg/kg 14 days resulted in substantial block of tumor growth and a 21-day tumor growth delay, with ERK phosphorylation inhibited by 43% in treated tumors, in COLO205 xenograft model[1]. | ||
| 作用机制 | PLX4720 is an ATP competitive kinase inhibitor.[1] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| 23132-87 | Growth Inhibition Assay | IC50=19.7642 μM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=20.0478 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=3.55266 μM | SANGER | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.42mL 0.48mL 0.24mL |
12.08mL 2.42mL 1.21mL |
24.16mL 4.83mL 2.42mL |
