GP-82996 (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 (apoptosis)。GP-82996可用于癌症研究。
| 生物活性 | GP-82996 (CINK4) is a pharmacological inhibitor ofCDK4/6. GP-82996 hasIC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces theapoptosisofcancercells U2OS. GP-82996 can be used in the research ofcancer[1][2]. |
| IC50& Target[1] | Cdk4/cyclin D1 1.5 μM (IC50) | CDK6/cyclinD1 5.6 μM (IC50) | CDK5/p35 25 μM (IC50) | CDK2/cyclinA >50 μM (IC50) | CDK1/cyclinB >100 μM (IC50) | CDK2/cyclin E >50 μM (IC50) | CDK4/cyclin D2 >50 μM (IC50) | Cdk6/cyclin D2 >50 μM (IC50) | V-abl >10 μM (IC50) | c-met >10 μM (IC50) | IGF-1R >10 μM (IC50) | Insulin-R >10 μM (IC50) |
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体外研究
(In Vitro) | 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 changes in the levels of CDK4 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 IC50values 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].
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体内研究
(In Vivo) | GP-82996 (30 mg/kg, i.p. for 29 days) shows 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 mm3)[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. |
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| 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. |
| 溶解性数据 | In Vivo: 1. 5% DMSO, 0.05% Tween 80, and 95% physiologic saline
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