cdk9 in 10

CDK9-IN-10 是一种有效的 CDK9 抑制剂。CDK9-IN-10 是 PROTAC CDK9 degrader-2 的配体。

CDK9 10 GSK3β-IN-1 是一种激酶抑制剂 (Flavopiridol 类似物)，能有效抑制 HsGSK3β、HsCDK9 CyclinT、HsCDK5 p25 和 HsCDK2 CyclinA，其 IC50 值分别为 59 nM、64 nM、1.093 μM 和 1.725 μM。CDK9 10 GSK3β-IN-1 表现出相当或高于 Flavopiridol 的抗癌细胞活性，在体外对多达七种癌细胞系表现出高抗增殖活性。

CDK9-IN-40 是一种 CDK2 (Cyclin dependent kinase 2) 抑制剂，其 IC50 对 CDK2 Cyclin E1 的抑制效能为 ≤ 10 nM。

CDK12-IN-2 (CDK12 inhibitor 2) 是一种有效的选择性 CDK12 抑制剂，对 CDK12、CDK2、CDK7 和 CDK9 的 IC50 为 52 nM、>100 μM、>10 μM 和 16 μM。 CDK12-IN-2可用于研究CDK12的功能。

EGFR HER2 CDK9-IN-3 (Compound 10) 是一种有效的 EGFR (IC50: 191.08 nM)、HER2 (IC50: 132.65 nM) 和 CDK9 (IC50: 113.98 nM) 抑制剂。EGFR HER2 CDK9-IN-3 表现出明显的抗肿瘤作用。

AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4 6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity.

AG-012986 HCl is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4 6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 HCl showed antiproliferative activities in vitro with IC(50)s of <100 nmol L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 HCl was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 HCl also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity.

QR-6401是一种口服、选择性的大环CDK2抑制剂，其IC50分别针对CDK2 E1、CDK9 T1、CDK1 A2、CDK6 D3和CDK4 D1为0.37、10、22、34及45nM。在OVCAR3卵巢癌异种移植模型中，QR-6401表现出显著的抗肿瘤活性，显示出其作为癌症研究工具的潜能。

CDK9-IN-28（化合物10）是一种高效CDK9抑制剂，可用作PROTAC合成中的靶蛋白配体，并在实体瘤中展现出显著的抗增殖能力。