产品
编 号：F753900
分子式：C25H20Cl2N6O3
分子量：523.37
分子式：C25H20Cl2N6O3
分子量：523.37
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CAS No: 2580938-58-3
产品详情
生物活性：
CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy.
体内研究：
CDK/HDAC-IN-2 (12.5, 25 mg/kg; IP; once daily for 21 days) shows antitumor efficacyin the HCT116 xenograft model (TGI= 51.0%).Pharmacokinetic Parameters of CDK/HDAC-IN-2 in ICR male mice.compound7c
Dose (mg/kg)20
administrationi.p.
t1/2 (h)2.61
Tmax (h)2.00
Cmax (h)7570
AUC0-∞ (ng h/mL)30700
MRT0-∞ (ng h/mL)3.31
F (%)63.6
ICR male mice; 20 mg/kg, i.p..Animal Model:ICR male mice
Dosage:20 mg/kg
Administration:IP
Result:Showed good Pharmacokinetic parameters with bioavailability of F= 63.6%.
Animal Model:5-6 weeks, BALB/c female mice (HCT116 xenograft nude mice models)
Dosage:12.5, 25 mg/kg
Administration:IP, once daily for 21 days
Result:Effectively inhibited the growth of HCT116 xenograft tumors tumor growth inhibitions (TGI) at 12.5 and 25 mg/kg of 37.0% and 51.0%, respectively.
体外研究：
CDK/HDAC-IN-2 (compound 7c) shows antiproliferative activity with IC50s of 0.71, 1.20, 1.83, 4.19, 7.76, 4.47 μM for HCT116, A375, Hela, H460, SMMC7721, NIH 3T3 cells, respectively.CDK/HDAC-IN-2 (24 h) shows anti-migration ability in A375 and H460 cells.CDK/HDAC-IN-2 (0.5, 1, 2 μM) induces apoptosis and cell cycle arrest at G2/M phase.CDK/HDAC-IN-2 accelerates intracellular ROS accumulation, leading to cancer cell death.
CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy.
体内研究：
CDK/HDAC-IN-2 (12.5, 25 mg/kg; IP; once daily for 21 days) shows antitumor efficacyin the HCT116 xenograft model (TGI= 51.0%).Pharmacokinetic Parameters of CDK/HDAC-IN-2 in ICR male mice.compound7c
Dose (mg/kg)20
administrationi.p.
t1/2 (h)2.61
Tmax (h)2.00
Cmax (h)7570
AUC0-∞ (ng h/mL)30700
MRT0-∞ (ng h/mL)3.31
F (%)63.6
ICR male mice; 20 mg/kg, i.p..Animal Model:ICR male mice
Dosage:20 mg/kg
Administration:IP
Result:Showed good Pharmacokinetic parameters with bioavailability of F= 63.6%.
Animal Model:5-6 weeks, BALB/c female mice (HCT116 xenograft nude mice models)
Dosage:12.5, 25 mg/kg
Administration:IP, once daily for 21 days
Result:Effectively inhibited the growth of HCT116 xenograft tumors tumor growth inhibitions (TGI) at 12.5 and 25 mg/kg of 37.0% and 51.0%, respectively.
体外研究：
CDK/HDAC-IN-2 (compound 7c) shows antiproliferative activity with IC50s of 0.71, 1.20, 1.83, 4.19, 7.76, 4.47 μM for HCT116, A375, Hela, H460, SMMC7721, NIH 3T3 cells, respectively.CDK/HDAC-IN-2 (24 h) shows anti-migration ability in A375 and H460 cells.CDK/HDAC-IN-2 (0.5, 1, 2 μM) induces apoptosis and cell cycle arrest at G2/M phase.CDK/HDAC-IN-2 accelerates intracellular ROS accumulation, leading to cancer cell death.
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