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编 号：F335783
分子式：C27H32N6O
分子量：456.58
分子式：C27H32N6O
分子量：456.58
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CAS No: 359886-84-3
产品详情
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.
体内研究：
GP-82996 (30 mg/kg, i.p. for 29 days) shows smaller final tumor volume compared with vehicle control in mouse xenograft models.Animal Model:19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm3)
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.
体外研究：
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.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.GP-82996 (5, 10 μM; 48 hours) induces aooptosis in 83% of U2OS cells in concentration of 10μM.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.GP-82996 (3, 5, 10 μM; 48 hours) induces G1 arrest in A549 and H23 cells.GP-82996 ((1, 3, 5, 10 μM; 72 hours) enhances Paclitaxel sensitivity in KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23 cells) .GP-82996 (10 μM; 72 hours) combined with Paclitaxel (3 nM; 72 hours) increases the apoptosis of A549 and H23 cells.
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.
体内研究：
GP-82996 (30 mg/kg, i.p. for 29 days) shows smaller final tumor volume compared with vehicle control in mouse xenograft models.Animal Model:19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm3)
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.
体外研究：
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.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.GP-82996 (5, 10 μM; 48 hours) induces aooptosis in 83% of U2OS cells in concentration of 10μM.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.GP-82996 (3, 5, 10 μM; 48 hours) induces G1 arrest in A549 and H23 cells.GP-82996 ((1, 3, 5, 10 μM; 72 hours) enhances Paclitaxel sensitivity in KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23 cells) .GP-82996 (10 μM; 72 hours) combined with Paclitaxel (3 nM; 72 hours) increases the apoptosis of A549 and H23 cells.
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