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HDAC1/2 and CDK2-IN-1
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HDAC1/2 and CDK2-IN-1
CAS No. : 2418559-01-8
MCE 站:HDAC1/2 and CDK2-IN-1
产品活性:HDAC1/2 and CDK2-IN-1 (compound 14d) 是一种有效的 HDAC1,HDAC2 和 CDK2 抑制剂,IC50 分别为 70.7,23.1 和 0.80 μM。HDAC1/2 and CDK2-IN-1 可阻断细胞周期,诱导细胞凋亡 (apoptosis)。HDAC1/2 and CDK2-IN-1 表现出良好的体内抗肿瘤活性。
研究领域:Cell Cycle/DNA Damage | Epigenetics | Apoptosis
In Vitro: 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.
In Vivo: 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 |
Administration | IV | IP |
T1/2 (h) | 1.48 | 2.84 |
Tmax (h) | 2 | |
Cmax (ng/mL) | 1360 | |
AUC0-t (ng/mL*h) | 2850 | 7240 |
MRT0-t (h) | 0.563 | 4.54 |
CL (mL/(min/kg)) | 23.3 | |
F (%) | 50.8 |
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