BTK-IN-7

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BTK-IN-7 

BTK-IN-7 是一种有效的选择性 BTK 抑制剂 (IC50=4.0 nM)，BTK-IN-7在酶 (ITK >250-fold, EGFR >2500-fold) 和细胞水平 (ITK >227-fold, EGFR 27-fold) 都具有较高的选择性。BTK-IN-7还具有较高的抗肿瘤活性。

BTK-IN-7

BTK-IN-7 Chemical Structure

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生物活性

BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels(ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity[1].

体外研究
(In Vitro)

BTK-IN-7 (compound 24a; 10, 100, 1000, 10000 nM; 48 hours) displays the antiproliferative effects in U-937 cells (IC50=3.6 μM)[1]. BTK-IN-7 (10, 100, 1000, 10000 nM; 48 hours; U937 cells) induces cell cycle arrest at the G1 phase in a concentration-dependent manner[1]. BTK-IN-7 (1-5 μM; 48 hours) induces apoptosis in U-937 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: U937, Ramos, Pfeiffer, Jeko-1 cells
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: 48 hours
Result: Displayed antiproliferative effects in U-937 (IC50=3.6 μM) cells.

Cell Cycle Analysis[1]

Cell Line: U937 cells
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: 48 hours
Result: Cells were arrested atthe G1 phase in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: U937 cells
Concentration: 1, 2.5, 5 μM
Incubation Time: 48 hours
Result: An apoptosis rate was increased to 22.75% at a concentration of 5 μM.

体内研究
(In Vivo)

BTK-IN-7 (25 and 50 mg/kg; intraperitoneal injection; daily for 14 days) inhibits tumor growth in a dose-dependent manner in U-937 xenograft mouse model, and 50 mg/kg dosage displays a better antitumor effect. BTK-IN-7 does not show significant parenchymal injury or inflammatory cell infiltration in organs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c nude mice (U397 xenograft mouse model) [1]
Dosage: 25, 50 mg/kg
Administration: Intraperitoneal injection; daily for 14 days
Result: Inhibited tumor growth in a dose-dependent manner and did not reveal significant parenchymal injury or inflammatory cell infiltration in organs.

分子量

540.61

Formula

C30H32N6O4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Dou D, et al. Discovery of Pteridine-7(8H)-one Derivatives as Potent and Selective Inhibitors of Bruton’s Tyrosine Kinase (BTK). J Med Chem. 2022;65(3):2694-2709.

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