PLX 4720 is a potent and selective inhibitor of B-RafV600E (IC50=13 nM) and c-Raf-1Y340D/Y341D (IC50=6.7 nM), whth a 10-fold selectivity for B-RafV600E than wild-type B-Raf.
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产品名称 | A-raf ↓ ↑ | B-Raf ↓ ↑ | C-Raf/Raf-1 ↓ ↑ | Raf ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Encorafenib | ✔ | 99%+ | |||||||||||||||||
GDC-0879 |
++++
B-Raf, IC50: 0.13 nM |
99%+ | |||||||||||||||||
SB-590885 |
++++
B-Raf, Ki: 0.16 nM |
99%+ | |||||||||||||||||
RAF265 | 99%+ | ||||||||||||||||||
Dabrafenib |
++++
B-Raf, IC50: 5.2 nM B-Raf (V600E), IC50: 0.7 nM |
+++
C-Raf, IC50: 6.3 nM |
98% | ||||||||||||||||
Lifirafenib |
++++
WT A-RAF, IC50: 1 nM |
++
BRAF WT, IC50: 32 nM BRAF(V600E), IC50: 23 nM |
+++
C-RAF (Y340/341D), IC50: 7 nM |
EGFR | 98% | ||||||||||||||
ZM 336372 |
+
C-Raf, IC50: 70 nM |
99%+ | |||||||||||||||||
NVP-BHG 712 |
+
C-Raf, IC50: 0.395 μM |
99%+ | |||||||||||||||||
CCT196969 |
+
BRAF, IC50: 0.1 μM |
++
CRAF, IC50: 0.01 μM |
Src | 98% | |||||||||||||||
Vemurafenib |
++
B-Raf, IC50: 100 nM B-Raf (V600E), IC50: 31 nM |
+
C-Raf, IC50: 48 nM |
98+% | ||||||||||||||||
PLX4720 |
++
B-Raf, IC50: 160 nM B-Raf (V600E), IC50: 13 nM |
+++
C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM |
BRK | 99+% | |||||||||||||||
GW 5074 |
+++
C-Raf, IC50: 9 nM |
99%+ | |||||||||||||||||
Avutometinib |
+++
BRAF, IC50: 19 nM BRAF V600E, IC50: 8.2 nM |
+
CRAF, IC50: 56 nM |
98% | ||||||||||||||||
LY3009120 |
++++
BRAF WT, IC50: 15 nM BRAF(V600E), IC50: 5.8 nM |
++++
C-Raf, IC50: 4.3 nM |
99%+ | ||||||||||||||||
Agerafenib |
++
B-Raf (V600E), Kd: 14 nM B-Raf, Kd: 36 nM |
+
C-Raf, Kd: 39 nM |
RET | 99%+ | |||||||||||||||
TAK-632 |
+++
B-Raf, IC50: 8.3 nM |
++++
C-Raf, IC50: 1.4 nM |
99%+ | ||||||||||||||||
AZ 628 |
+
B-Raf, IC50: 105 nM B-Raf (V600E), IC50: 34 nM |
++
C-Raf-1, IC50: 29 nM |
99% | ||||||||||||||||
PLX7904 | ✔ | 98+% | |||||||||||||||||
Sorafenib |
++
B-Raf, IC50: 22 nM B-Raf (V599E), IC50: 38 nM |
++++
Raf-1, IC50: 6 nM |
++++
Raf-1, IC50: 6 nM |
99% | |||||||||||||||
Tovorafenib | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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 | ||
786-0 | Growth Inhibition Assay | IC50=45.65 μM | SANGER | ||
Dose | Mice: 5 mg/kg - 20 mg/kg, max = 1000 mg/kg[1] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 918505-84-7 |
分子式 | C17H14ClF2N3O3S |
分子量 | 413.826 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
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 |