化学信息：
| 化学名 | 4-[8-amino-3-[(2S)-1-but-2-ynoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-N-pyridin-2-ylbenzamide |
|
| 简称 | ACP-196 | |
| 别名 |
Acalabrutinib |
|
| 中文名 | N/A | |
| 化学式 | C26H23N7O2 | |
| 分子量 | 465.51 | |
| CAS号 | 1420477-60-6 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO93mg/ml; Ethanol93mg/ml |
|
| 溶液配制 | 5mg加入1.07ml DMSO，或者每4.66mg加入1ml DMSO，配制成10mM溶液。SC1072-10mM用DMSO配制。 |
生物信息：
| 产品描述 | Acalabrutinib is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. | ||||
| 信号通路 | Angiogenesis | ||||
| 靶点 | BTK | － | － | － | － |
| IC50 | 3nM | － | － | － | － |
| 体外研究 | In the in vitro signaling assay on primary human CLL cells, acalabrutinib inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT. Acalabrutinib demonstrates higher selectivity for BTK with IC50 determinations on nine kinases with a cysteine residue in the same position as BTK. Importantly, unlike ibrutinib, acalabrutinib does not inhibit EGFR, ITK, or TEC. acalabrutinib has no effect on EGFR phosphorylation on tyrosine residues Y1068 and Y1173. Compared with ibrutinib, acalabrutinib has much higher IC50 (>1000nM) or virtually no inhibition on kinase activities of ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1. | ||||
| 体内研究 | oral administration of ACP-196 in mice results in dose-dependent inhibition of anti-IgM-induced CD86 expression in CD19+ splenocytes with an ED50 of 0.34mg/kg compared to 0.91mg/kg for ibrutinib. A similar model is used to compare the duration of Btk inhibition after a single oral dose of 25mg/kg. ACP-196 inhibits CD86 expression >90% at 3h postdose. | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | primary human CLL cells, T cells, NK cells and epithelial cells |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | canine model of B cell NHL |
| 配制 | N/A |
| 剂量 | 2.5, 5, 10mg/kg. |
| 给药方式 | orally administered |
| 产品编号 | 产品名称 | 包装 |
| SC1072-10mM | ACP-196 (BTK抑制剂) | 10mM×0.2ml |
| SC1072-5mg | ACP-196 (BTK抑制剂) | 5mg |
| SC1072-25mg | ACP-196 (BTK抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
