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编 号：F756509
分子式：C28H28FN5O2
分子量：485.55
分子式：C28H28FN5O2
分子量：485.55
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CAS No: 2872677-61-5
产品详情
生物活性：
CDK9-IN-22 is a potent CDK9 inhibitor with IC50s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity.
体内研究：
CDK9-IN-22 (5, 10, 20 mg/kg; i.p.; every other day for four weeks) 抑制异种移植小鼠模型中的肿瘤生长。Animal Model:BALB/c nude mice (PANC-1 tumor xenograft murine model)
Dosage:5, 10, 20 mg/kg
Administration:I.p.; every other day for four weeks
Result:Inhibited the tumor growth with the tumor inhibition rate (TIR) was 6.2, 32.6 and 54.2% at the dose of 5, 10 and 20 mg/kg, respectively.
体外研究：
CDK9-IN-22 (compound 8 d) (0.1, 0.5, 2.5 μM; 24, 48 h) 在 PANC-1 细胞中以浓度依赖性方式诱导细胞凋亡和细胞周期停滞在 G2/M 期[1 ].CDK9-IN-22 (0.1, 0.5, 2.5 μM; 24 h) 降低 PANC-1 细胞中 p-RNAPII (S2) 和 CDK9 蛋白的表达。
CDK9-IN-22 is a potent CDK9 inhibitor with IC50s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity.
体内研究：
CDK9-IN-22 (5, 10, 20 mg/kg; i.p.; every other day for four weeks) 抑制异种移植小鼠模型中的肿瘤生长。Animal Model:BALB/c nude mice (PANC-1 tumor xenograft murine model)
Dosage:5, 10, 20 mg/kg
Administration:I.p.; every other day for four weeks
Result:Inhibited the tumor growth with the tumor inhibition rate (TIR) was 6.2, 32.6 and 54.2% at the dose of 5, 10 and 20 mg/kg, respectively.
体外研究：
CDK9-IN-22 (compound 8 d) (0.1, 0.5, 2.5 μM; 24, 48 h) 在 PANC-1 细胞中以浓度依赖性方式诱导细胞凋亡和细胞周期停滞在 G2/M 期[1 ].CDK9-IN-22 (0.1, 0.5, 2.5 μM; 24 h) 降低 PANC-1 细胞中 p-RNAPII (S2) 和 CDK9 蛋白的表达。
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