896720-20-0|VX-11e|CsnPharm

CAS No.: 896720-20-0

VX-11e Catalog No. CSN18540

Synonyms: VTX-11e;Vertex-11e;TCS ERK 11e

VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK (Extracellular Signal-Regulated Kinase) and is antitumor agent.

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400-920-2911

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技术信息

生物活性

描述Extracellular signal-regulated kinases (ERKs) are protein kinase intracellular signaling molecules that participate in Ras-Raf-MEK-ERK signal transduction cascade, which is related with the regulation of various processes including cell adhesion, cell cycle progression, cell migration, cell survival, differentiation, metabolism, proliferation, and transcription^[3]. VX-11e is an ERK inhibitor with IC50 value of 17 nM and 15 nM on ERK1 and ERK2, respectively^[4]. While VX-11e was tested for cytotoxic activity on A549 and DM122, they EC50 value is 770 nM and 370 nM after four days of incubation. The ERK1/2 phosphorylation level analyzed by western blot assay showed enhancement at both 0.5 μM and 2μM of vx-11e^[4]. In human melanoma RPDX tumor expanded NSG mice, the vx-11e was given 50 mg/kg BID for 2 weeks. VX-11 could inhibit the tumor growth significantly compared to control, and the PI3K expression level measured by western blot assay was inhibited in the tumor tissue^[5].
作用机制The vx-11e can bind with the inactive, unphosphorylated and active, phosphorylated ERK2. The equilibrium between the T and R-state conformers formed by the inhibitor with the inactive and active enzyme is strongly shifts to favor the R form. Thus, the allosteric properties of ERK2 endow the active form of the kinase with a novel capability of being inhibited through mechanisms involving conformational selection^[6].
细胞研究
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
HT-29 cells - Proliferation assay - Antiproliferative activity against human HT-29 cells, IC50=0.048 μM 19827834
动物研究
剂量
Mice: 50 mg/kg^[1] (p.o., BID)

给药途径
p.o.
参考文献

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HT-29 cells	-	Proliferation assay	-	Antiproliferative activity against human HT-29 cells, IC50=0.048 μM	19827834

动物研究
剂量	Mice: 50 mg/kg^[1] (p.o., BID)
给药途径	p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9986 mL
- 9.9930 mL
- 19.9859 mL
- 5 mM
- 0.3997 mL
- 1.9986 mL
- 3.9972 mL
- 10 mM
- 0.1999 mL
- 0.9993 mL
- 1.9986 mL

技术信息

CAS号

896720-20-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H20Cl2FN5O2

运输

蓝冰

分子量

500.35

别名

VTX-11e;Vertex-11e;TCS ERK 11e;TCS Extracellular Signal-Related Kinase 11e;ERK-11e

溶解度

DMSO	330.0 mg/mL (659.5 mM)
Water	insoluble

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