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
CAS: 745833-23-2
产品质控
批次：
纯度：
99.63%
99.63
VX-702相关产品
相关信号通路图
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 |
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| 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] |
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|---|---|---|---|---|
| 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，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，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) | |||
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体外溶解度 |
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 |
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体内溶解度 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
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
只
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，注：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：取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：取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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