产品
编 号：F752300
分子式：C31H43N9O2
分子量：573.73
分子式：C31H43N9O2
分子量：573.73
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CAS No: 2412707-81-2
产品详情
生物活性：
PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity.
体内研究：
PLK1/BRD4-IN-1 (9b) (60 mg/kg/d; IG; 18 days) results in a significant decrease in average tumor size, with no obvious toxicity.Animal Model:Five weeks old male NOD-SCID mice.
Dosage:60 mg/kg/d
Administration:Oral gavage, 18 days; tumor xenograft models were established by subcutaneously injecting 100 μL of 1×108 cell/mL MV4-11 cell suspension into NOD-SCID mice.
Result:Resulted in a significant decrease in average tumor size, with 66% tumor growth inhibition, and didn’t obviously affect the body weight of mice.
体外研究：
PLK1/BRD4-IN-1 (9b) (72 h) shows broad-spectrum antiproliferative activities.PLK1/BRD4-IN-1 (0-9 μM, 24 h) induces cell cycle arrest.PLK1/BRD4-IN-1 (0-9 μM, 48 h) induces cell apoptosis.PLK1/BRD4-IN-1 inhibits the proliferative of cancer cells by exerting its inhibitory activity on both PLK1 and BRD4.
PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity.
体内研究：
PLK1/BRD4-IN-1 (9b) (60 mg/kg/d; IG; 18 days) results in a significant decrease in average tumor size, with no obvious toxicity.Animal Model:Five weeks old male NOD-SCID mice.
Dosage:60 mg/kg/d
Administration:Oral gavage, 18 days; tumor xenograft models were established by subcutaneously injecting 100 μL of 1×108 cell/mL MV4-11 cell suspension into NOD-SCID mice.
Result:Resulted in a significant decrease in average tumor size, with 66% tumor growth inhibition, and didn’t obviously affect the body weight of mice.
体外研究：
PLK1/BRD4-IN-1 (9b) (72 h) shows broad-spectrum antiproliferative activities.PLK1/BRD4-IN-1 (0-9 μM, 24 h) induces cell cycle arrest.PLK1/BRD4-IN-1 (0-9 μM, 48 h) induces cell apoptosis.PLK1/BRD4-IN-1 inhibits the proliferative of cancer cells by exerting its inhibitory activity on both PLK1 and BRD4.
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