VX-702

VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.

VX-702化学構造

CAS No. 745833-23-2

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 298500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(38)

製品安全説明書

現在のバッチを見る: 純度: 99.63%
99.63

VX-702関連製品

シグナル伝達経路

p38 MAPK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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生物活性

製品説明 VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.
特性 Highly selective, orally active inhibitor of p38 MAPK.
Targets
p38α [1]
(Cell-free assay)
4 nM-20 nM
In Vitro
In vitro

Pre-incubation of platelets with VX-702 (1 μM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen. VX-702 shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or absence of anti-platelet therapies. [1] VX-702 inhibits the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner. [2]

In Vivo
In Vivo

The half-life of VX-702 is 16 to 20 hours, with a median clearance of 3.75 L/h and a volume of distribution of 73 L/kg. Both AUC and Cmax values are dose proportional for VX-702, which is predominantly cleared renally. [2] VX-702 (at a dose of 0.1 mg/kg twice daily) has an equivalent effect. In addition, VX-702 (5 mg/kg twice daily) , as measured by percentage inhibition of wrist joint erosion and inflammation score. [3] VX-702 selectively inhibits activation of p38 MAPK after ischemia with no effects on ERKs and JNKs. The MI/AAR ratio is significantly reduced in the 50 mg/kg group compared with the 5 mg/kg and vehicle groups.[4]

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

化学情報

分子量 404.3 化学式

C19H12F4N4O2

CAS No. 745833-23-2 SDF Download VX-702 SDFをダウンロードする
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
保管

In vitro
Batch:

DMSO : 81 mg/mL ( (200.34 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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