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VX-702

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Chemical Structure| 745833-23-2 同义名 : -
CAS号 : 745833-23-2
货号 : A756758
分子式 : C19H12F4N4O2
纯度 : 99%+
分子量 : 404.318
MDL号 : MFCD11616590
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(98.93 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 9 mg/mL clear

PO 0.5% CMC-Na 75 mg/mL suspension

生物活性
靶点

  • p38α

    p38α, IC50:4 nM-20 nM
描述 The stress-activated protein kinase (SAPK) p38 isoforms are mitogen-activated protein kinase (MAPK) family members. MAPKs act as an integration point for multiple biochemical signals, and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation and development. The well reported isoforms of p38 MAPKs include p38α, p38β and others. VX-702 is a selective inhibitor of p38α MAPK. VX-702 inhibited the activation of platelet MAPK-activated protein kinase-2, the substrate of p38α MAPK with IC50s ranging from 4 – 20 nM[3]. In an ex vivo blood assay primed with LPS, VX-702 dose-dependently inhibited the production of IL-6, IL-1β and TNFα with IC50s of 59, 122 and 99 ng/ml, respectively [4]. In collagen-induced mouse arthritis model, VX-702 dosed at 0.1 mg/kg twice daily or 5 mg/kg twice daily were of equivalent therapeutic effects to methotrexate or prednisolone at the same doses, as measured by the percentage inhibition of wrist joint erosion and an inflammation score[4]. In a rat model of ischemia-reperfusion injury, VX-702 orally administrated at the doses of 5 or 50 mg/kg dose-dependently reduced the increase of phosphor MK2 in the ischemic zone tissue, and the MI/AAR ratio was significantly reduced in the 50 mg/kg VX-702 treated group[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.01543 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 A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=7.80384 μM SANGER
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.37mL

2.47mL

1.24mL

24.73mL

4.95mL

2.47mL
参考文献

[1]Naka K, Jomen Y, et al. Dipeptide species regulate p38MAPK-Smad3 signalling to maintain chronic myelogenous leukaemia stem cells. Nat Commun. 2015 Aug 20;6:8039.

[2]Kuliopulos A, Mohanlal R, et al. Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation. Thromb Haemost. 2004 Dec;92(6):1387-93.

[3]Kuliopulos A, Mohanlal R, Covic L. Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation. Thromb Haemost. 2004 Dec;92(6):1387-93.

[4]Ding C. Drug evaluation: VX-702, a MAP kinase inhibitor for rheumatoid arthritis and acute coronary syndrome. Curr Opin Investig Drugs. 2006 Nov;7(11):1020-5.