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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C19H12F4N4O2 |
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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) |
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* <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. |
製品説明 | VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. |
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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 | 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 as that of methotrexate (0.1 mg/kg). In addition, VX-702 (5 mg/kg twice daily) also has an equivalent effect as prednisolone (10 mg/kg once 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] |
特徴 | Highly selective, orally active inhibitor of p38 MAPK. |
動物実験 | 動物モデル | Mouse with collagen-induced arthritis |
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投薬量 | ≤10 mg/kg | |
投与方法 | Administered via p.o. |
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]
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 |
The Blockade of Tumoral IL1β-Mediated Signaling in Normal Colonic Fibroblasts Sensitizes Tumor Cells to Chemotherapy and Prevents Inflammatory CAF Activation [ Int J Mol Sci, 2021, 22(9)4960] | PubMed: 34066976 |
Dual Inhibition of AKT and MEK Pathways Potentiates the Anti-Cancer Effect of Gefitinib in Triple-Negative Breast Cancer Cells [ Cancers (Basel), 2021, 13(6)1205] | PubMed: 33801977 |
P38 mitogen activated protein kinase inhibitor improves platelet in vitro parameters and in vivo survival in a SCID mouse model of transfusion for platelets stored at cold or temperature cycled conditions for 14 days [ PLoS One, 2021, 16(5):e0250120] | PubMed: 33974660 |
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] | PubMed: 32645325 |
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] | PubMed: 32645325 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。