VX-745 selectively inhibits p38¦Á and p38¦Â MAPK with IC50 of 10 nM and 220 nM, respectively, but not p38¦Ã MAPK and a large panel of other kinases, with IC50 larger than 20 µM. In a human peripheral blood mononuclear cell (PBMC) assay, VX-745 provides IC50 of 56 and 52 nM for IL-1¦Â and TNF¦Á, respectively. VX-745 blocks IL-6 and IL-8 production induced by IL-1 and TNF¦Á, and COX-2 synthesis mediated by LPS and IL-1¦Â. VX-745 (60 nM-20 µM) inhibits IL-6 and VEGF secretion in bone marrow stromal cells (BMSCs), without affecting their viability. VX-745 also inhibits TNF-¦Á-induced IL-6 secretion in BMSCs. VX-745 inhibits both multiple myeloma (MM) cell proliferation and IL-6 secretion in BMSCs triggered by adherence of MM cells to BMSCs, suggesting that VX-745 can inhibit paracrine multiple myeloma (MM) cell growth in the BM milieu and overcome cell adhesion-related drug resistance.

June 21, 2017

prudect name : VX-745 selectively inhibits p38¦Á and p38¦Â MAPK with IC50 of 10 nM and 220 nM, respectively, but not p38¦Ã MAPK and a large panel of other kinases, with IC50 larger than 20 µM. In a human peripheral blood mononuclear cell (PBMC) assay, VX-745 provides IC50 of 56 and 52 nM for IL-1¦Â and TNF¦Á, respectively. VX-745 blocks IL-6 and IL-8 production induced by IL-1 and TNF¦Á, and COX-2 synthesis mediated by LPS and IL-1¦Â. VX-745 (60 nM-20 µM) inhibits IL-6 and VEGF secretion in bone marrow stromal cells (BMSCs), without affecting their viability. VX-745 also inhibits TNF-¦Á-induced IL-6 secretion in BMSCs. VX-745 inhibits both multiple myeloma (MM) cell proliferation and IL-6 secretion in BMSCs triggered by adherence of MM cells to BMSCs, suggesting that VX-745 can inhibit paracrine multiple myeloma (MM) cell growth in the BM milieu and overcome cell adhesion-related drug resistance.
VX-745

Synonyms: CAS NO: 209410-46-8Molecular Formula: C₁₉H₉Cl₂F₂N₃OSMolecular Weight: 436.26Purity: 98% minSolubility: In DMSOStorage: -20°C

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