VX-702

目錄號：S6005 Purity: 99.63%

VX-702是一種高選擇性p38α MAPK抑制劑，作用于p38α比作用于p38β效果高14倍。

VX-702 Chemical Structure

CAS: 745833-23-2

規(guī)格	價格	庫存
10mM (1mL in DMSO)	647.01	現(xiàn)貨
10mg	575.24	現(xiàn)貨
100mg	3023.34	現(xiàn)貨
1g	18591.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.63%

99.63

VX-702相關(guān)產(chǎn)品

相關(guān)靶點	p38α p38β	點擊展開
相關(guān)產(chǎn)品	Adezmapimod (SB203580) SB202190 Doramapimod (BIRB 796) Ralimetinib (LY2228820) dimesylate PH-797804 Losmapimod SB239063 Neflamapimod (VX-745) BMS-582949 Skepinone-L Asiatic Acid TAK-715 Pamapimod Pexmetinib SD 0006 R1487 PD 169316	點擊展開
相關(guān)化合物庫	激酶抑制劑庫 MAPK抑制劑庫細胞周期化合物庫 TGF-beta/Smad信號通路庫抗阿爾茨海默病化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	活性描述	文獻信息
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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

VX-702是一種高選擇性p38α MAPK抑制劑，作用于p38α比作用于p38β效果高14倍。

特性

VX-702是高選擇性，口服有效的p38 MAPK 抑制劑。

靶點

p38α ^[1]
(Cell-free assay)

4 nM-20 nM

體外研究(In Vitro)
體外研究活性	用1 μM VX-702處理血小板，完全或局部抑制由血小板興奮劑(包括凝血酵素, SFLLRN, AYPGKF, U46619, 和膠原)誘導(dǎo)的p38活性,IC50為4到20 nM。VX-702作用于p38 MAPK興奮劑誘導(dǎo)的血小板聚集沒有效果。^[1]VX-702 抑制IL-6, IL-1β和TNFα 的產(chǎn)生，IC50分別為59, 122和99 ng/ml，這種作用存在劑量依賴性。^[2]

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	VX-702半衰期為16到20小時,半數(shù)清除劑量3.75 L，分布容積為73 L/kg。 ^[2]VX-702按0.1 mg/kg劑量每天處理兩次，按0.1 mg/kg劑量處理效果差不多。此外，VX-702按5 mg/kg劑量每天處理兩次，測定腕關(guān)節(jié)病變和炎癥抑制百分數(shù)。^[3] VX-702選擇性抑制p38 MAPK活性，對ERKs和JNKs沒有抑制效果。按50-mg/kg劑量處理的實驗組與對照組和按5-mg/kg劑量處理實驗組相比，MI/AAR比率明顯降低。^[4]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00395577	Completed	Rheumatoid Arthritis	Vertex Pharmaceuticals Incorporated	November 2006	Phase 2

參考文獻
[1] Kuliopulos A, et al. Thromb Haemost, 2004, 92(6), 1387-1393. [2] Braddock M, IDDB Meeting Report, 2005, March 14-15. [3] Gill A, IDDB Meeing Report, 2002, March 06-08. [4] Bhattacharya K, et al. Circulation, 2003, 108(17), 882. + 展開

參考文獻

[1] Kuliopulos A, et al. Thromb Haemost, 2004, 92(6), 1387-1393.
[2] Braddock M, IDDB Meeting Report, 2005, March 14-15.
[3] Gill A, IDDB Meeing Report, 2002, March 06-08.

[4] Bhattacharya K, et al. Circulation, 2003, 108(17), 882.

+ 展開

化學(xué)信息&溶解度

分子量	404.3	分子式	C₁₉H₁₂F₄N₄O₂
CAS號	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
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 81 mg/mL ( (200.34 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 81 mg/mL ( (200.34 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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* 必填項

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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