Product Introduction
Bioactivity


英文名: GP-82996

描述: GP-82996 (CINK4) (CINK4) 是 CDK4/6的药理学抑制剂。GP-82996 对 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35 的 IC50s 分别为 1.5、5.6 和 25 μM。GP-82996 诱导肿瘤细胞 U2OS 的凋亡，可用于癌症研究。

体外活性: GP-82996 (5, 10 μM; 24 hours) induces G1 arrest and G0-G1/S ratio increase in U2OS (p16 negative) and MRC-5 (p16 positive) cells [1]. GP-82996 (5, 10 μM; 24 hours) reduces hyperphosphorylation of pRb, but has no effect on CDK4 levels in U2OS, MRC-5 cells [1]. GP-82996 (5, 10 μM; 48 hours) induces aooptosis in 83% of U2OS cells in concentration of 10μM [1]. GP-82996 (0.1-40 μM; 24,48, 72 hours) inhibits the cell proliferation of A549, H358, SKLU-1, H23, PC14 cells with IC 50 values of 72 h are 4-7 μM [2]. GP-82996 (3, 5, 10 μM; 48 hours) induces G1 arrest in A549 and H23 cells [2]. GP-82996 ((1, 3, 5, 10 μM; 72 hours) enhances Paclitaxel sensitivity in KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23 cells) [2]. GP-82996 (10 μM; 72 hours) combined with Paclitaxel (3 nM; 72 hours) increases the apoptosis of A549 and H23 cells [2].

体内活性: GP-82996 (30 mg/kg, i.p. for 29 days) exhibits smaller final tumor volume compared with vehicle control in mouse xenograft models [1]. Animal Model: 19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm 3 ) [1] Dosage: 30 mg/kg Administration: i.p. every 12 hours for 29 days Result: Showed smaller final tumor volume compared with vehicle control in mouse xenograft models.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 27mg/mL (59.1mM)


关键字: GP82996 | CINK-4 | GP 82996 | CINK 4 | GP-82996

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相关库: Anti-Breast Cancer Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library