R406
| CAS号 | 841290-80-0 | 货号 | BCP01933 |
| 中文名 | R406 | ||
| 英文名 | R406 | ||
| 中文别名 | |||
| 英文别名 | R-406;R 406;R406 free base;Tamatinib; | ||
| 分子式 | C22H23FN6O5 | 分子量 | 470.45 |
| 生物活性 | R406 is an ATP-competitive inhibitor of Syk with a Ki value of 30 nM. R406 selectively inhibits Syk-dependent signaling with EC50 values ranging from 33 nM to 171 nM, more potently than Syk-independent pathways in different cells.R406 inhibits cellular proliferation of a large panel of diffuse large B-cell lymphoma (DLBCL) cell lines at EC50 values ranging from 0.8 μM to 8.1 μM. R406 treatment (1 μM or 4 μM) induces the activation of caspases 9 and 3, but not caspase 8, leading to significant apoptosis of the majority of DLBCL cell lines. Pretreatment of R406 completely blocks the phosphorylation of SYK525/526 and the SYK-dependent phosphorylation of BLNK in R406-sensitive DLBCLs following B-cell receptor (BCR) crosslinking. R406 potently decreases MMP-9 mRNA levels by 2.8- and 4.3-fold lower than controls after 24 and 48 hours treatment, respectively, and reduces the invasive capacity of the RL cells. | ||
| 上下游产品 | 841290-81-1（R406苯磺酸盐） | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase | ||
| 靶 点 | Syk | ||
结构式
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