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| Cas No.: | 745833-23-2 |
| Chemical Name: | 1-(5-carbamoyl-6-(2,4-difluorophenyl)pyridin-2-yl)-1-(2,6-difluorophenyl)urea |
| Synonyms: | vx 702 |
| SMILES: | O=C(N)C1=CC=C(N=C1C2=CC=C(C=C2F)F)N(C3=C(C=CC=C3F)F)C(N)=O |
| Formula: | C19H12F4N4O2 |
| M.Wt: | 404.3 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | VX-702 is a highly selective inhibitor of p38α MAPK(IC50=4 -20 nM), 14-fold higher potency against the p38α versus p38β |
| Target: | IC50 value: 4-20 nM [1] Target: p38α MAPK |
| 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]. |
| 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]. |
| References: | [1]. Kuliopulos A, et al. Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation. 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]. Naka K, et al. Dipeptide species regulate p38MAPK-Smad3 signalling to maintain chronic myelogenous leukaemia stem cells. Nat Commun. 2015 Aug 20;6:8039. |
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