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BTK
Bruton's tyrosine kinase (BTK) belongs to the Tec kinases family of tyrosine protein kinases. It is a crucial terminal kinase in the B cell receptor (BCR) signaling pathway, and essential for the development and activation of B cells. Aberrant activation of B cells is found to play a central role in the pathogenesis of B-cell lymphomas and autoimmune diseases. BTK is involved in multiple signaling pathways,and plays an important role in the B-cell receptor (BCR) signal pathway, including the PI3K, MAPK and NF-κB pathways. After BCR is first activated by phosphorylation, phosphorylated BCR recruits spleen tyrosine kinase (SYK) to the membrane, where SYK is phosphorylated and subsequently phosphorylates BTK. Activated BTK can phosphorylate PLCγ2 in Y753 and Y759, which is critical for lipase activity. BTK may be a potential target for therapy of hematological malignancies and autoimmune diseases.
References
1.Feng Y,et al. Expert Opin Ther Pat. 2019 Apr;29(4):217-241.
References
1.Feng Y,et al. Expert Opin Ther Pat. 2019 Apr;29(4):217-241.
Tyrosine Kinase
BTK
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JAK3/BTK-IN-1
产品货号 : M37669
cas no: 2674036-91-8
JAK3/BTK-IN-1 是一种有效的 JAK3/BTK 抑制剂。BTK 和 JAK3 是自身免疫性疾病的两个重要靶点。同时抑制 BTK/JAK3 信号通路表现出协同效应。JAK3/BTK-IN-1具有研究J AK3 激酶和/或 BTK 相关疾病的潜力 (摘自专利 WO2021147952A1，化合物 002)。
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TAK-020
产品货号 : M37633
cas no: 1627603-21-7
TAK-020 是一种Btk共价抑制剂，成为临床候选活性分子。
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BLK degrader 1
产品货号 : M36930
cas no: 3049215-64-4
BLK degrader 1 is a selective B lymphoid tyrosine kinase (BLK) degrader with anticancer activity and can be used for cancer research.
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NX-2127
产品货号 : M36530
cas no: 2416131-46-7
NX-2127 是一种口服有效的 BTK 抑制剂，可诱导细胞中突变的 BTKC481S 降解。NX-2127 抑制 BTKC481S 突变体 TMD8 细胞的增殖，比 Ibrutinib (HY-10997) 更有效。NX-2127 催化 Ikaros (IKZF1) 和 Aiolos (IKZF3) 的降解，对应的作用浓度分别为 25 nM 和 54 nM。NX-2127 刺激 T 细胞活化并增加原代人 T 细胞中 IL-2 的产生。
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BGB-8035
产品货号 : M36520
cas no: 2283349-24-4
BGB-8035 是一种口服有效，高选择性 BTK 抑制剂，对 BTK、TEC、EGFR 的 IC50 分别为 1.1 nM、99 nM、621 nM。BGB-8035 具有抗肿瘤和抗关节炎活性。BGB-8035 具有用于 B 细胞恶性肿瘤和自身免疫性疾病研究的潜力。
