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首页-小分子抑制剂&激动剂-Tyrosine Kinase-ITK-Soquelitinib
Soquelitinib

Chemical Structure : Soquelitinib

CAS No.: 2226636-04-8

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Soquelitinib (CPI-818, CPI818)

货号: PC-26224Not For Human Use, Lab Use Only.

Soquelitinib (CPI-818) is a selective, covalent, orally bioavailable inhibitor of ITK kinase (Interleukin-2-inducible T cell kinase) with Kd of 6.5 nM, >80-fold selective over other TEC kinase family members, binds covalently to cysteine 442 of ITK and blocks its function.

规格 价格 库存 数量
5 mg ￥2180 In stock
10 mg ￥3480 In stock
25 mg ￥5480 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Soquelitinib (CPI-818) is a selective, covalent, orally bioavailable inhibitor of ITK kinase (Interleukin-2-inducible T cell kinase) with Kd of 6.5 nM, >80-fold selective over other TEC kinase family members, binds covalently to cysteine 442 of ITK and blocks its function.
Soquelitinib displays >100-fold selectivity compared to binding to resting lymphocyte kinase (RLK).
Soquelitinib inhibits TCR signaling downstream of ITK and blocks IL-2 production, suppresses IL-2 secretion in Jurkat cells in response to TCR stimulation with a mean IC50 of 136 nM.
Soquelitinib suppresses Th2 associated cytokines and induces Th1 skewing in CD4 T cells.
Soquelitinib inhibits tumor growth and enhances cytolytic capacity of tumor infiltrating T cells.
Soquelitinib enhances anti-PD1 and anti-CTLA4 efficacy in the CT26 tumor model.
Soquelitinib inhibits T cell exhaustion process in vitro.

物理化学性质&存储条件

分子量 514.66
分子式 C25H30N4O4S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-N-(5-((5-(4-Acryloyl-3-methyl-1,4-diazepane-1-carbonyl)-4-methoxy-2-methylphenyl)thio)thiazol-2-yl)cyclopropanecarboxamide

参考文献

1. Hsu L Y, et al. bioRxiv, 2023: 2023.10. 27.564296.

2. Hsu L Y, et al. bioRxiv, 2023: 2023.07. 05.547822.

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