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CDK9-IN-22
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CDK9-IN-22图片
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
CDK9-IN-22 是一种有效的CDK9抑制剂，对 CDK9 和 CDK 的IC50分别为 10.4、876.2 nM。CDK9-IN-22 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G2/M 期。CDK9-IN-22 降低 p-RNAPII (S2) 和 CDK9 蛋白的表达。CDK9-IN-22 具有抗增殖和抗肿瘤活性。
生物活性

CDK9-IN-22 is a potentCDK9inhibitor withIC50s of 10.4, 876.2 nM forCDK9,CDK, respectively. CDK9-IN-22 inducesapoptosisand cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) andCDK9protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity[1].

IC50& Target[1]

CDK9/cyclinT1

10.4 nM (IC50)

cdk2/cyclin A

876.2 nM (IC50)

体外研究
(In Vitro)

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[1]。

Cell Proliferation Assay[1]

Cell Line:A549, H1975, A431, PANC-1, HCT-116, LO2 cells
Concentration:0-100 μM
Incubation Time:72 h
Result:Showed antiproliferative activity with IC50s of 0.66, 0.43, 0.10, 0.08, 0.09, 1.43 μM for A549, H1975, A431, PANC-1, HCT-116, LO2 cells, respectively.

Apoptosis Analysis[1]

Cell Line:PANC-1 cells
Concentration:0.1, 0.5, 2.5 μM
Incubation Time:48 h
Result:Induced apoptosis with the percentage of total apoptotic cells was 43.6, 54.1 and 65.8% at 0.1, 0.5 and 2.5 μM, respectively.

Cell Cycle Analysis[1]

Cell Line:PANC-1 cells
Concentration:0.1, 0.5, 2.5 μM
Incubation Time:24 h
Result:Arrested the cell cycle at the G2/M phase in a dose-dependent manner (21.83% for 0.1 μM, 25.85% for 0.5 μM and 34.26% for 2.5 μM).

Western Blot Analysis[1]

Cell Line:PANC-1 cells
Concentration:0.1, 0.5, 2.5 μM
Incubation Time:24 h
Result:Decreased the expression of p-RNAPII (S2) and CDK9 protein in a dose-dependent manner.
体内研究
(In Vivo)

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[1]。

Animal Model:BALB/c nude mice (PANC-1 tumor xenograft murine model)[1]
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.
分子量

485.55

Formula

C28H28FN5O2

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.