VX-702

VX-702是一种高选择性p38α MAPK抑制剂,作用于p38α比作用于p38β效果高14倍。

VX-702 Chemical Structure

VX-702 Chemical Structure

CAS: 745833-23-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 647.01 现货
10mg RMB 575.24 现货
100mg RMB 3023.34 现货
200mg RMB 5477.38 现货
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客户使用Selleck的VX-702发表文献37

产品质控

批次: 纯度: 99.63%
99.59

VX-702相关产品

相关信号通路图

p38 MAPK抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.01543 μM SANGER
human NCI-H720 cell Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=0.01682 μM SANGER
JVM-2 cell Growth inhibition assay Inhibition of human JVM-2 cell growth in a cell viability assay, IC50=0.083 μM SANGER
human NCI-H69 cell Growth inhibition assay Inhibition of human NCI-H69 cell growth in a cell viability assay, IC50=0.09941 μM SANGER
human BV-173 cell Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50=0.11386 μM SANGER
human KU812 cell Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=0.12488 μM SANGER
human DU-145 cell Growth inhibition assay Inhibition of human DU-145 cell growth in a cell viability assay, IC50=0.14554 μM SANGER
KARPAS-45 cell Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=0.14826 μM SANGER
human AGS cell Growth inhibition assay Inhibition of human AGS cell growth in a cell viability assay, IC50=0.15251 μM SANGER
human MOLT-13 cell Growth inhibition assay Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=0.15981 μM SANGER
human NCI-H209 cell Growth inhibition assay Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50=0.1758 μM SANGER
human CTV-1 cell Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=0.18389 μM SANGER
LU-139 cell Growth inhibition assay Inhibition of human LU-139 cell growth in a cell viability assay, IC50=0.19435 μM SANGER
ML-2 cell Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50=0.22661 μM SANGER
human K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay, IC50=0.22917 μM SANGER
human SBC-1 cell Growth inhibition assay Inhibition of human SBC-1 cell growth in a cell viability assay, IC50=0.2362 μM SANGER
human COR-L88 cell Growth inhibition assay Inhibition of human COR-L88 cell growth in a cell viability assay, IC50=0.3348 μM SANGER
human KY821 cell Growth inhibition assay Inhibition of human KY821 cell growth in a cell viability assay, IC50=0.39603 μM SANGER
human HCC2218 cell Growth inhibition assay Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=0.49728 μM SANGER
human ECC10 cell Growth inhibition assay Inhibition of human ECC10 cell growth in a cell viability assay, IC50=0.65389 μM SANGER
human EW-3 cell Growth inhibition assay Inhibition of human EW-3 cell growth in a cell viability assay, IC50=0.66611 μM SANGER
human EW-18 cell Growth inhibition assay Inhibition of human EW-18 cell growth in a cell viability assay, IC50=0.74679 μM SANGER
human UACC-257 cell Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=1.20326 μM SANGER
human G-361 cell Growth inhibition assay Inhibition of human G-361 cell growth in a cell viability assay, IC50=1.49519 μM SANGER
human HMV-II cell Growth inhibition assay Inhibition of human HMV-II cell growth in a cell viability assay, IC50=1.77184 μM SANGER
human DEL cell Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay, IC50=2.20704 μM SANGER
human IGROV-1 cell Growth inhibition assay Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=2.43188 μM SANGER
human SK-OV-3 cell Growth inhibition assay Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=2.61697 μM SANGER
human LAMA-84 cell Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=2.71284 μM SANGER
human NCI-H510A cell Growth inhibition assay Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50=2.92526 μM SANGER
human CP66-MEL cell Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=2.93559 μM SANGER
human HAL-01 cell Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=3.27918 μM SANGER
human RS4-11 cell  Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=3.70573 μM SANGER
human RPMI-8226 cell Growth inhibition assay Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50=3.82376 μM SANGER
human NCI-H82 cell Growth inhibition assay Inhibition of human NCI-H82 cell growth in a cell viability assay, IC50=3.89305 μM SANGER
human NY cells Growth inhibition assay Inhibition of human NY cell growth in a cell viability assay, IC50=4.27637 μM SANGER
human MDA-MB-361 cell Growth inhibition assay Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=4.43158 μM SANGER
human MOLT-4 cell Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=4.99193 μM SANGER
human DU-4475 cell Growth inhibition assay Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=5.05565 μM SANGER
human ESS-1 cell Growth inhibition assay Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=5.29179 μM SANGER
human NCI-H1299 cell Growth inhibition assay Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=5.53033 μM SANGER
human COLO-684 cell Growth inhibition assay Inhibition of human COLO-684 cell growth in a cell viability assay, IC50=5.58165 μM SANGER
human MV-4-11 cell Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=5.71199 μM SANGER
human D-542MG cell Growth inhibition assay Inhibition of human D-542MG cell growth in a cell viability assay, IC50=6.39272 μM SANGER
human A4-Fuk cell Growth inhibition assay Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=6.43662 μM SANGER
human HL-60 cell Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50=7.52212 μM SANGER
human NCI-H526 cell Growth inhibition assay Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50=7.59801 μM SANGER
human L-363 cell Growth inhibition assay Inhibition of human L-363 cell growth in a cell viability assay, IC50=7.79252 μM SANGER
human A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=7.80384 μM SANGER
human MS-1 Growth inhibition assay Inhibition of human MS-1 cell growth in a cell viability assay, IC50=7.83465 μM SANGER
human JAR cell Growth inhibition assay Inhibition of human JAR cell growth in a cell viability assay, IC50=7.84923 μM SANGER
human TI-73 cell Growth inhibition assay Inhibition of human TI-73 cell growth in a cell viability assay, IC50=8.0622 μM SANGER
human CTB-1 cell Growth inhibition assay Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=8.17825 μM SANGER
human SK-NEP-1 cell Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=11.3038 μM SANGER
human HT-29 cell Growth inhibition assay Inhibition of human HT-29 cell growth in a cell viability assay, IC50=13.9111 μM SANGER
human NCI-H1092 cell Growth inhibition assay Inhibition of human NCI-H1092 cell growth in a cell viability assay, IC50=14.318 μM SANGER
human KMOE-2 cell Growth inhibition assay Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50=14.6178 μM SANGER
human EM-2 cell Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50=15.2841 μM SANGER
human RT-112 cell Growth inhibition assay Inhibition of human RT-112 cell growth in a cell viability assay, IC50=15.3984 μM SANGER
human DB cell Growth inhibition assay Inhibition of human DB cell growth in a cell viability assay, IC50=15.8513 μM SANGER
human NCI-H1770 cell Growth inhibition assay Inhibition of human NCI-H1770 cell growth in a cell viability assay SANGER
human CAL-54 cell Growth inhibition assay Inhibition of human CAL-54 cell growth in a cell viability assay, IC50=16.73 μM SANGER
human NB14 cell Growth inhibition assay Inhibition of human NB14 cell growth in a cell viability assay, IC50=17.6395 μM SANGER
human RPMI-7951 cell Growth inhibition assay Inhibition of human RPMI-7951 cell growth in a cell viability assay, IC50=19.1783 μM SANGER
human T47D cell Growth inhibition assay Inhibition of human T47D cell growth in a cell viability assay, IC50=21.2243 μM SANGER
human A549 cell Growth inhibition assay Inhibition of human A549 cell growth in a cell viability assay, IC50=21.2811 μM SANGER
human A2780 cell Growth inhibition assay Inhibition of human A2780 cell growth in a cell viability assay, IC50=21.8225 μM SANGER
human SK-MEL-24 cell Growth inhibition assay Inhibition of human SK-MEL-24 cell growth in a cell viability assay, IC50=33.0311 μM SANGER
点击查看更多细胞系数据

生物活性

产品描述 VX-702是一种高选择性p38α MAPK抑制剂,作用于p38α比作用于p38β效果高14倍。
特性 VX-702是高选择性,口服有效的p38 MAPK 抑制剂。
靶点
p38α [1]
(Cell-free assay)
4 nM-20 nM
体外研究(In Vitro)
体外研究活性

用1 μM VX-702处理血小板,完全或局部抑制由血小板兴奋剂(包括凝血酵素, SFLLRN, AYPGKF, U46619, 和胶原)诱导的p38活性,IC50为4到20 nM。VX-702作用于p38 MAPK兴奋剂诱导的血小板聚集没有效果。[1]VX-702 抑制IL-6, IL-1β和TNFα 的产生,IC50分别为59, 122和99 ng/ml,这种作用存在剂量依赖性。[2]

体内研究(In Vivo)
体内研究活性

VX-702半衰期为16到20小时,半数清除剂量3.75 L,分布容积为73 L/kg。 [2]VX-702按0.1 mg/kg剂量每天处理两次,与methotrexate 按0.1 mg/kg剂量处理效果差不多。此外,VX-702按5 mg/kg剂量每天处理两次,与prednisolone按10 mg/kg剂量每天处理一次,效果差不多,测定腕关节病变和炎症抑制百分数。[3] VX-702选择性抑制p38 MAPK活性,对ERKs和JNKs没有抑制效果。按50-mg/kg剂量处理的实验组与对照组和按5-mg/kg剂量处理实验组相比,MI/AAR比率明显降低。[4]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00395577 Completed
Rheumatoid Arthritis
Vertex Pharmaceuticals Incorporated
November 2006 Phase 2

化学信息&溶解度

分子量 404.3 分子式

C19H12F4N4O2

CAS号 745833-23-2 SDF Download VX-702 SDF
Smiles C1=CC(=C(C(=C1)F)N(C2=NC(=C(C=C2)C(=O)N)C3=C(C=C(C=C3)F)F)C(=O)N)F
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 81 mg/mL ( 200.34 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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