Emavusertib
| CAS号 | 1801344-14-8 | 货号 | BCP33271 |
| 中文名 | Emavusertib | ||
| 英文名 | Emavusertib | ||
| 中文别名 | |||
| 英文别名 | CA 4948; CA4948;CA-4948; | ||
| 分子式 | C24H25N7O5 | 分子量 | 491.51 |
| 生物活性 | Emavusertib is an orally bioavailable, reversible inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4), with potential antineoplastic, immunomodulating and anti-inflammatory activities. Upon oral administration, emavusertib targets, binds to, and blocks the kinase activity of IRAK4. This inhibits IRAK4-mediated signaling, prevents the activation of IRAK4-mediated nuclear factor-kappa B (NF-kB) signaling and decreases the expression of inflammatory cytokines and certain pro-survival factors. This inhibits proliferation of IRAK4-overactivated tumor cells, which are found in cells harboring MYD88 activating mutations or those with overactivated toll-like receptor (TLR) pathways. In addition, CA-4948 may inhibit inflammation and immune-mediated cell destruction in inflammatory and auto-immune diseases where TLR or interleukin 1 receptor (IL-1R) signaling is overactivated and MYD88 is dysregulated. IRAK4, a serine/threonine-protein kinase that plays a key role in both the TLR and IL-1R signaling pathways, is activated though the adaptor protein MYD88 and links the TLR and IL-1R signaling pathway to the NF-kB pathway. | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase | ||
| 靶 点 | IRAK FLT3 | ||
结构式
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