VX-702

製品コードS6005 バッチS600504

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H12F4N4O2
分子量 404.3 CAS No. 745833-23-2
Solubility (25°C)* 体外 DMSO 81 mg/mL (200.34 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
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. This compound shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or absence of anti-platelet therapies. [1] It 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

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 this compound, which is predominantly cleared renally. [2] This compound (at a dose of 0.1 mg/kg twice daily) has an equivalent effect. In addition, this chemical (5 mg/kg twice daily) , as measured by percentage inhibition of wrist joint erosion and inflammation score. [3] It 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]
特徴 Highly selective, orally active inhibitor of p38 MAPK.

プロトコル(参考用のみ)

動物実験 動物モデル Mouse with collagen-induced arthritis
投薬量 ≤10 mg/kg
投与方法 Administered via p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/15583748/
  • http://eprints.utas.edu.au/3610/1/vx-702.pdf
  • http://eprints.utas.edu.au/3610/1/vx-702.pdf
  • http://circ.ahajournals.org/content/108/17.toc

カスタマーフィードバック

Data from [Mol Immunol, 2014, 62(2), 266-76]

, , Lee lay hoon from National University of Singapore

Data from [Data independently produced by , , J Invest Dermatol, 2018, 138(6):1380-1390]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Spatial covariance reveals isothiocyanate natural products adjust redox stress to restore function in alpha-1-antitrypsin deficiency [ Cell Rep Med, 2025, 6(1):101917] PubMed: 39809267
Type 1 interferon signalling orchestrated by gut microbiota suppresses IgE-mediated anaphylaxis associated with vitamin D3 signalling [ World Allergy Organ J, 2025, 18(8):101089] PubMed: 40697952
Stress Response Kinase MK2 Induces Non-canonical Activation of EphA2 in EML4-ALK Lung Cancer Cells [ Biol Pharm Bull, 2025, 48(2):172-176] PubMed: 40024717
Distinct cAMP regulation in scleroderma lung and skin myofibroblasts governs their dedifferentiation via p38α inhibition [ bioRxiv, 2025, 2025.02.26.640163] PubMed: 40060695
Cooperative induction of CXCL chemokines by inflammatory cytokines and oxidized phospholipids [ Immunology, 2024, 10.1111/imm.13773] PubMed: 38468451
Coadaptation fostered by the SLIT2-ROBO1 axis facilitates liver metastasis of pancreatic ductal adenocarcinoma [ Nat Commun, 2023, 14(1):861] PubMed: 36792623
Inhibition of p38 signaling curtails the SARS-CoV-2 induced inflammatory response but retains the IFN-dependent antiviral defense of the lung epithelial barrier [ Antiviral Res, 2022, 209:105475] PubMed: 36423831
Epstein-Barr virus-induced ectopic CD137 expression helps nasopharyngeal carcinoma to escape immune surveillance and enables targeting by chimeric antigen receptors [ Cancer Immunol Immunother, 2022, 10.1007/s00262-022-03183-8] PubMed: 35299256
Inhibition of IκB Kinase Is a Potential Therapeutic Strategy to Circumvent Resistance to Epidermal Growth Factor Receptor Inhibition in Triple-Negative Breast Cancer Cells [ Cancers (Basel), 2022, 14(21)5215] PubMed: 36358633
5-fluorouracil suppresses stem cell-like properties by inhibiting p38 in pancreatic cancer cell line PANC-1 [ Folia Histochem Cytobiol, 2022, 10.5603/FHC.a2022.0004] PubMed: 35103981

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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