产品
编 号：F754102
分子式：C24H25F3N6O4S
分子量：550.55
分子式：C24H25F3N6O4S
分子量：550.55
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CAS No: 2622273-55-4
产品详情
生物活性：
PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma.
体内研究：
PLK1-IN-4 exhibits low metabolic stability in species of human, mouse, dog and monkey, with CLhep of 74.3, 330.9, 61.5 and 196.5 mL/min/kg, respectively.PLK1-IN-4 (30 mg/kg; tail vein injection; once or twice daily, for 12 days) suppresses tumor growth in a dose dependent manner.Pharmacokinetic Parameters of PLK1-IN-4 in male ICR mouse.IV (5 mg/kg)
C0 (ng/mL)1790
T1/2 (h)1.47
MRT0-inf (h)0.808
MRT0-t (h)0.704
AUC0-t (ng·h/mL)767
AUC0-inf (ng·h/mL)776
CL (mL/min/kg)107
VdSS (L/kg)107
Animal Model:Male nu/nu BALB/c mice (4-6 weeks; injected with HepG2 cells)
Dosage:30 mg/kg
Administration:Tail vein injection; once or twice daily, for 12 days
Result:Suppressed tumor growth in a dose dependent manner, and the tumor growth inhibition (TGI) values were 120.0% and 135.2% at doses of 30 mg/kg once daily and 30 mg/kg twice daily, respectively.
Animal Model:ICR mouse
Dosage:5 mg/kg
Administration:IV; single (Pharmacokinetics Analysis)
Result:Exhibited a short half-life (T1/2) of 1.47 h, moderate exposure with an area under the curve (AUC0-inf) of 776 ng·h/mL and volume of distribution at steady state (Vdss) of 5.21 L/kg.
体外研究：
PLK1-IN-4 (compound 31) (0-5 μM; 48 hours) exhibits excellent antiproliferative activities against HCC cells.PLK1-IN-4 (60 and 100 nM; 24 hours) induces abnormal spindle formation in HepG2 and HT-29 cells.PLK1-IN-4 (10-300 nM; 0-48 hours) induces apoptosis in cancer cells through G2/M arrest.PLK1-IN-4 (0-120 nM; 24 hours) increases phosphorylation of PLK1, histone H3 and NPM and decreases phosphorylation of Cdc2 in a dose-dependent manner.
PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma.
体内研究：
PLK1-IN-4 exhibits low metabolic stability in species of human, mouse, dog and monkey, with CLhep of 74.3, 330.9, 61.5 and 196.5 mL/min/kg, respectively.PLK1-IN-4 (30 mg/kg; tail vein injection; once or twice daily, for 12 days) suppresses tumor growth in a dose dependent manner.Pharmacokinetic Parameters of PLK1-IN-4 in male ICR mouse.IV (5 mg/kg)
C0 (ng/mL)1790
T1/2 (h)1.47
MRT0-inf (h)0.808
MRT0-t (h)0.704
AUC0-t (ng·h/mL)767
AUC0-inf (ng·h/mL)776
CL (mL/min/kg)107
VdSS (L/kg)107
Animal Model:Male nu/nu BALB/c mice (4-6 weeks; injected with HepG2 cells)
Dosage:30 mg/kg
Administration:Tail vein injection; once or twice daily, for 12 days
Result:Suppressed tumor growth in a dose dependent manner, and the tumor growth inhibition (TGI) values were 120.0% and 135.2% at doses of 30 mg/kg once daily and 30 mg/kg twice daily, respectively.
Animal Model:ICR mouse
Dosage:5 mg/kg
Administration:IV; single (Pharmacokinetics Analysis)
Result:Exhibited a short half-life (T1/2) of 1.47 h, moderate exposure with an area under the curve (AUC0-inf) of 776 ng·h/mL and volume of distribution at steady state (Vdss) of 5.21 L/kg.
体外研究：
PLK1-IN-4 (compound 31) (0-5 μM; 48 hours) exhibits excellent antiproliferative activities against HCC cells.PLK1-IN-4 (60 and 100 nM; 24 hours) induces abnormal spindle formation in HepG2 and HT-29 cells.PLK1-IN-4 (10-300 nM; 0-48 hours) induces apoptosis in cancer cells through G2/M arrest.PLK1-IN-4 (0-120 nM; 24 hours) increases phosphorylation of PLK1, histone H3 and NPM and decreases phosphorylation of Cdc2 in a dose-dependent manner.
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