产品
编 号：F762873
分子式：C26H29ClN8O3S
分子量：569.08
分子式：C26H29ClN8O3S
分子量：569.08
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CAS No: 3033549-18-4
产品详情
生物活性：
ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALKWT, ALKL1196M and ALKG1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity.
体内研究：
ALK-IN-23 notes a moderate half-life of 16.3 min and a high intrinsic liver clearance of 152.9 mL/min/kg in rats.ALK-IN-23 (25 and 50 mg/kg; IG; once every 2 days; for 14 days) exhibited gentle antitumor efficacy and no significant weight loss in H2228 xenograft mice model.Animal Model:Female BALB/c nude mice (5×106 cells H2228 cells suspended in serum-free media were injected into the flanks)
Dosage:25 and 50 mg/kg
Administration:IG; once every 2 days; for 14 days
Result:Presented moderate antitumor efficacy with the tumor growth inhibition (TGI) of 70.46% at 50 mg/kg.Possessed gentle antitumor efficacy and exhibited no significant weight loss.
体外研究：
ALK-IN-23 (compound Y28) (0-5 μM; 72h) has highly inhibitory activity against H3122, H2228, Karpas299 and A549.ALK-IN-23 (25-100 nM; 3 days) clearly reduces the number of H2228 cell colonies, and almost completely abolishes the formation of colonies at 100 nM.ALK-IN-23 (100-200 nM; 48 h) facilitates the apoptosis of H2228 cells.ALK-IN-23 (5-10 nM; 24 and 48 h) is effective to block the migration of most cells at a dose of 10 nM.ALK-IN-23 (25-100 nM; overnight) significantly increases the percentage of cells in the G2 phase.
ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALKWT, ALKL1196M and ALKG1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity.
体内研究：
ALK-IN-23 notes a moderate half-life of 16.3 min and a high intrinsic liver clearance of 152.9 mL/min/kg in rats.ALK-IN-23 (25 and 50 mg/kg; IG; once every 2 days; for 14 days) exhibited gentle antitumor efficacy and no significant weight loss in H2228 xenograft mice model.Animal Model:Female BALB/c nude mice (5×106 cells H2228 cells suspended in serum-free media were injected into the flanks)
Dosage:25 and 50 mg/kg
Administration:IG; once every 2 days; for 14 days
Result:Presented moderate antitumor efficacy with the tumor growth inhibition (TGI) of 70.46% at 50 mg/kg.Possessed gentle antitumor efficacy and exhibited no significant weight loss.
体外研究：
ALK-IN-23 (compound Y28) (0-5 μM; 72h) has highly inhibitory activity against H3122, H2228, Karpas299 and A549.ALK-IN-23 (25-100 nM; 3 days) clearly reduces the number of H2228 cell colonies, and almost completely abolishes the formation of colonies at 100 nM.ALK-IN-23 (100-200 nM; 48 h) facilitates the apoptosis of H2228 cells.ALK-IN-23 (5-10 nM; 24 and 48 h) is effective to block the migration of most cells at a dose of 10 nM.ALK-IN-23 (25-100 nM; overnight) significantly increases the percentage of cells in the G2 phase.
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