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CGP-82996 (Synonyms: CINK4)
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。
CGP-82996 Chemical Structure
CAS No. : 359886-84-3
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer[1][2].
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| IC50 & Target[1] |
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Cdk4/cyclin D1
1.5 μM (IC50)
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CDK6/cyclinD1
5.6 μM (IC50)
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CDK5/p35
25 μM (IC50)
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CDK2/cyclinA
>50 μM (IC50)
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CDK1/cyclinB
>100 μM (IC50)
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CDK2/cyclin E
>50 μM (IC50)
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CDK4/cyclin D2
>50 μM (IC50)
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Cdk6/cyclin D2
>50 μM (IC50)
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V-abl
>10 μM (IC50)
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c-met
>10 μM (IC50)
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IGF-1R
>10 μM (IC50)
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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 IC50 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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 溶解性数据 |
In Vivo:
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1.
5% DMSO, 0.05% Tween 80, and 95% physiologic saline
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| 参考文献 |
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[1]. Soni R, et al. Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4. J Natl Cancer Inst. 2001 Mar 21;93(6):436-46.
[2]. Zhang XH, et al. A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS. Cancer Biol Ther. 2013;14(7):597-605.
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