产品
编 号：F762644
分子式：C30H32N6O4
分子量：540.61
分子式：C30H32N6O4
分子量：540.61
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CAS No: 2952702-39-3
产品详情
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.
体内研究：
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 shows significant parenchymal injury or inflammatory cell infiltration in organs.Animal Model:Male BALB/c nude mice (U397 xenograft mouse model)
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.
体外研究：
BTK-IN-7 (compound 24a; 10, 100, 1000, 10000 nM; 48 hours) displays the antiproliferative effects in U-937 cells (IC50=3.6 μM).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.BTK-IN-7 (1-5 μM; 48 hours) induces apoptosis in U-937 cells.
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.
体内研究：
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 shows significant parenchymal injury or inflammatory cell infiltration in organs.Animal Model:Male BALB/c nude mice (U397 xenograft mouse model)
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.
体外研究：
BTK-IN-7 (compound 24a; 10, 100, 1000, 10000 nM; 48 hours) displays the antiproliferative effects in U-937 cells (IC50=3.6 μM).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.BTK-IN-7 (1-5 μM; 48 hours) induces apoptosis in U-937 cells.
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