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PLX4720 {[allProObj[0].p_purity_real_show]}

货号:A332013

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.

PLX4720 化学结构 CAS号:918505-84-7
PLX4720 化学结构
CAS号:918505-84-7
PLX4720 3D分子结构
CAS号:918505-84-7
PLX4720 化学结构 CAS号:918505-84-7
PLX4720 3D分子结构 CAS号:918505-84-7
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PLX4720 纯度/质量文件 产品仅供科研

货号:A332013 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

PLX4720 生物活性

靶点
  • B-Raf

    B-Raf, IC50:160 nM

    B-Raf (V600E), IC50:13 nM

  • C-Raf/Raf-1

    C-Raf-1 (Y340D/Y341D), IC50:6.7 nM

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]

PLX4720 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
786-0 Growth Inhibition Assay IC50=45.65 μM SANGER

PLX4720 动物研究

Dose Mice: 5 mg/kg - 20 mg/kg, max = 1000 mg/kg[1] (p.o.)
Administration p.o.

PLX4720 实验方案

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

PLX4720 技术信息

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

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