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编 号：F752578
分子式：C26H22ClN7O
分子量：483.95
分子式：C26H22ClN7O
分子量：483.95
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CAS No: 2418559-01-8
产品详情
生物活性：
HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity.
体内研究：
HDAC1/2 and CDK2-IN-1 (BALB/c nude mice, 0-100 mg/kg, IP, once daily for 21 days) significantly inhibits the tumor growth.HDAC1/2 and CDK2-IN-1 (compound 14d) (ICR mice; 4 mg/kg, IV; 20 mg/kg, IP) exhibits desirable pharmacokinetic properties.Pharmacokinetic Parameters of HDAC1/2 and CDK2-IN-1 in male ICR mice.Dose (mg/kg)4 20
AdministrationIVIP
T1/2 (h)1.482.84
Tmax (h)2
Cmax (ng/mL)1360
AUC0-t (ng/mL*h)28507240
MRT0-t (h)0.5634.54
CL (mL/(min/kg))23.3
F (%)50.8
Animal Model:Male ICR mice (n = 9)
Dosage:4 mg/kg (IV), 20 mg/kg (IP)
Administration:IV, IP, once (Pharmacokinetic Analysis)
Result:Exhibited desirable pharmacokinetic properties.
Animal Model:BALB/c nude mice (5-6 weeks, HCT116 xenograft model)
Dosage:0, 25, 50 and 100 mg/kg
Administration:IP, once daily for 21 days
Result:Significantly inhibited the tumor growth, the tumor growth inhibitions were 28%, 40% and 44% at doses of 25, 50 and 100 mg/kg, respectively.
体外研究：
HDAC1/2 and CDK2-IN-1 (compound 14d) shows excellent antiproliferative activities against H460, A375, HepG2, HCT116 and Hela cells with IC50 values of 1.59, 0.47, 0.86, 0.58 and 1.05 μM, respectively.HDAC1/2 and CDK2-IN-1 (0.5 μM, 48 h) significantly inhibits the migration of H460 and A375 cells.HDAC1/2 and CDK2-IN-1 (0-2 μM, 24 h) significantly blocks the cell cycle in the G2/M phase.HDAC1/2 and CDK2-IN-1 (0-2 μM, 48 h) promotes cancer cell apoptosis in a dose-dependent manner.HDAC1/2 and CDK2-IN-1 (1 μM, 12 h) inhibits CDK2 and HDAC activity, causing cancer cell death.HDAC1/2 and CDK2-IN-1 (1 μM, 24 h) strongly increases ROS levels in A375 cells, causes cancer cell death by improving intracellular ROS levels.
HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity.
体内研究：
HDAC1/2 and CDK2-IN-1 (BALB/c nude mice, 0-100 mg/kg, IP, once daily for 21 days) significantly inhibits the tumor growth.HDAC1/2 and CDK2-IN-1 (compound 14d) (ICR mice; 4 mg/kg, IV; 20 mg/kg, IP) exhibits desirable pharmacokinetic properties.Pharmacokinetic Parameters of HDAC1/2 and CDK2-IN-1 in male ICR mice.Dose (mg/kg)4 20
AdministrationIVIP
T1/2 (h)1.482.84
Tmax (h)2
Cmax (ng/mL)1360
AUC0-t (ng/mL*h)28507240
MRT0-t (h)0.5634.54
CL (mL/(min/kg))23.3
F (%)50.8
Animal Model:Male ICR mice (n = 9)
Dosage:4 mg/kg (IV), 20 mg/kg (IP)
Administration:IV, IP, once (Pharmacokinetic Analysis)
Result:Exhibited desirable pharmacokinetic properties.
Animal Model:BALB/c nude mice (5-6 weeks, HCT116 xenograft model)
Dosage:0, 25, 50 and 100 mg/kg
Administration:IP, once daily for 21 days
Result:Significantly inhibited the tumor growth, the tumor growth inhibitions were 28%, 40% and 44% at doses of 25, 50 and 100 mg/kg, respectively.
体外研究：
HDAC1/2 and CDK2-IN-1 (compound 14d) shows excellent antiproliferative activities against H460, A375, HepG2, HCT116 and Hela cells with IC50 values of 1.59, 0.47, 0.86, 0.58 and 1.05 μM, respectively.HDAC1/2 and CDK2-IN-1 (0.5 μM, 48 h) significantly inhibits the migration of H460 and A375 cells.HDAC1/2 and CDK2-IN-1 (0-2 μM, 24 h) significantly blocks the cell cycle in the G2/M phase.HDAC1/2 and CDK2-IN-1 (0-2 μM, 48 h) promotes cancer cell apoptosis in a dose-dependent manner.HDAC1/2 and CDK2-IN-1 (1 μM, 12 h) inhibits CDK2 and HDAC activity, causing cancer cell death.HDAC1/2 and CDK2-IN-1 (1 μM, 24 h) strongly increases ROS levels in A375 cells, causes cancer cell death by improving intracellular ROS levels.
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