| SKU:K1299 | M. Wt:436.26 | ||
| Formula:C19H9Cl2F2N3OS | Solubility:No | ||
| Purity:>99% | Storage:2 years -20°C Powder | ||
| CAS No.:209410-46-8 | Synonyms:N/A | ||
| Chemical NameN/A | |||
| 供货周期： | 一周 |
| 品牌： | |
| 规格： | 2mg |
| 货号： | K1299 |
| CAS号： | 209410-46-8 |
| SKU:K1299 | M. Wt:436.26 | ||
| Formula:C19H9Cl2F2N3OS | Solubility:No | ||
| Purity:>99% | Storage:2 years -20°C Powder | ||
| CAS No.:209410-46-8 | Synonyms:N/A | ||
| Chemical NameN/A | |||
| Description | VX-745 | |||||
|---|---|---|---|---|---|---|
| Targets | p38-alpha MAPK | p38-beta MAPK | ||||
| IC50 | 10 nM | 220 nM | ||||
| In vitro | VX-745,a lead anti-inflammatory candidate, is a small-molecule inhibitor of mitogen-activated protein kinase (MAPK). VX-745 inhibits interleukin 6 (IL-6) and vascular endothelial growth factor (VEGF) secretion in bone marrow stromal cells (BMSCs), without affecting their viability. VX-745 can also inhibit tumor necrosis factor alpha (TNF-alpha)-induced IL-6 secretion in BMSCs. VX-745 inhibits both MM cell proliferation and IL-6 secretion in BMSCs triggered by adherence of MM cells to BMSCs. VX-745 can inhibit paracrine MM cell growth in the BM milieu and overcome cell adhesion-related drug resistance. VX-745 potently inhibited TNF release from LPS stimulated human THP-1 cells with IC50s of 29 nM. | |||||
| In vivo | VX-745 is effective against adjuvant-induced arthritis (AA) in the rat with ED50 of 5 mg/kg. Histological scores for VX-745 in AA rats are 93% inhibition of bone resorption and 56% inhibition of inflammation. | |||||
| Clinical Trials | N/A | |||||
| Features | N/A | |||||
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