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编 号：F754553
分子式：C25H28FN9
分子量：473.55
分子式：C25H28FN9
分子量：473.55
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CAS No: 2677026-14-9
产品详情
生物活性：
CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50?values of 39 and 88 nM, respectively.?CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity.
体内研究：
CDK6/PIM1-IN-1 (compound 51; orally; 60, 90 mg/kg/day; 17 days) displays more potent antitumor activity?in BALB/c mice with K562 cell lines. CDK6/PIM1-IN-1 (iv; 5 mg/kg) has the t1/2, MRT0-∞, and AUC0-∞?values of 9.78 h, 14.61 h, and 1153.74 h·ng/mL, respectively in Sprague–Dawley (SD) rats. CDK6/PIM1-IN-1 (po; 5 mg/kg) has the?t1/2, Tmax, Cmax, and AUC0-∞ of 15.81 h, 11 h, 152.31 ng/mL, and 5152.92 h·ng/mL, respectively in SD rats.
体外研究：
CDK6/PIM1-IN-1 (compound 51)?exhibits more than 10 times selectivity over CDK1 (IC50>10 μM), CDK2 (IC50=2.274 μM), CDK3 (IC50>10 μM), CDK5 (IC50>10 μM), CDK7 (IC50=393 nM), CDK9 (IC50=440 nM), CDK12 (IC50>10 μM), and CDK13 (IC50>10 μM). CDK6/PIM1-IN-1?shows inhibitory activity against PIM2 (IC50>10 μM) and PIM3 (IC50=92 nM). CDK6/PIM1-IN-1 inhibits proliferation in AML cells (K562 cell,GI50=1.026 μM; HL-60 cell,GI50=1.069 μM; MOLM13 cell, GI50=1.362 μM). CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM) causes a G1 arrest in a dose-dependent manner in K562 and HL-60 cell lines.CDK6/PIM1-IN-1?(1, 2, 4 μM) promotes the apoptosis of K562 and HL-60 cell lines in a dose-dependent manner. CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM; for 24 h) reduces?p-retinoblastoma (RB) and?p-BAD levels in a concentration-dependent manner. CDK6/PIM1-IN-1 decreases the PIM1 level.
CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50?values of 39 and 88 nM, respectively.?CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity.
体内研究：
CDK6/PIM1-IN-1 (compound 51; orally; 60, 90 mg/kg/day; 17 days) displays more potent antitumor activity?in BALB/c mice with K562 cell lines. CDK6/PIM1-IN-1 (iv; 5 mg/kg) has the t1/2, MRT0-∞, and AUC0-∞?values of 9.78 h, 14.61 h, and 1153.74 h·ng/mL, respectively in Sprague–Dawley (SD) rats. CDK6/PIM1-IN-1 (po; 5 mg/kg) has the?t1/2, Tmax, Cmax, and AUC0-∞ of 15.81 h, 11 h, 152.31 ng/mL, and 5152.92 h·ng/mL, respectively in SD rats.
体外研究：
CDK6/PIM1-IN-1 (compound 51)?exhibits more than 10 times selectivity over CDK1 (IC50>10 μM), CDK2 (IC50=2.274 μM), CDK3 (IC50>10 μM), CDK5 (IC50>10 μM), CDK7 (IC50=393 nM), CDK9 (IC50=440 nM), CDK12 (IC50>10 μM), and CDK13 (IC50>10 μM). CDK6/PIM1-IN-1?shows inhibitory activity against PIM2 (IC50>10 μM) and PIM3 (IC50=92 nM). CDK6/PIM1-IN-1 inhibits proliferation in AML cells (K562 cell,GI50=1.026 μM; HL-60 cell,GI50=1.069 μM; MOLM13 cell, GI50=1.362 μM). CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM) causes a G1 arrest in a dose-dependent manner in K562 and HL-60 cell lines.CDK6/PIM1-IN-1?(1, 2, 4 μM) promotes the apoptosis of K562 and HL-60 cell lines in a dose-dependent manner. CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM; for 24 h) reduces?p-retinoblastoma (RB) and?p-BAD levels in a concentration-dependent manner. CDK6/PIM1-IN-1 decreases the PIM1 level.
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