产品
编 号：F756306
分子式：C26H31ClN6O
分子量：479.02
分子式：C26H31ClN6O
分子量：479.02
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CAS No: 2841473-39-8
产品详情
生物活性：
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.
体内研究：
ZLMT-12 (compound 35; 10 mg/kg; p.o.; daily, for 21 d) has antitumor efficacy and inhibits tumor growth, without causing liver harm in the HCT116 xenograft model.Animal Model:Male BALB/cA-nu mice with HCT116 xenografts (18-25 g, 6-8 weeks of age)
Dosage:10 mg/kg
Administration:Oral administration; daily, for 21 days
Result:Inhibited tumor growth with GI (tumor volume growth inhibition)=47.66% and TGI (tumor weight growth inhibition)=62.39%.Exhibited no significant changes in behavior or body weight in mice.Had no obvious liver injury.
Animal Model:Male Sprague-Dawley rats (240±20 g)
Dosage:2 mg/kg (i.v.) and 20 mg/kg (p.o.) (Pharmacokinetic Analysis)
Administration:Intravenous injection and oral administration; once
Result:1.19Parameter2 mg/kg (i.v.)20 mg/kg (p.o.)
T1/2 (h)0.4611.77
Tmax (h)0.083/td>1.00
Cmax (ng/mL)20667.8
AUCo-t (h*ng/mL)110302
AUCo-∞ (h*ng/mL)115316
CL (L/h/kg)18.7
Vss(L/Kg)12.6
F (%)27.47
体外研究：
ZLMT-12 (compound 35; 500 nM; 72 h) has antiproliferative activity in cancer cells.ZLMT-12 (500 nM; 72 h) induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.
体内研究：
ZLMT-12 (compound 35; 10 mg/kg; p.o.; daily, for 21 d) has antitumor efficacy and inhibits tumor growth, without causing liver harm in the HCT116 xenograft model.Animal Model:Male BALB/cA-nu mice with HCT116 xenografts (18-25 g, 6-8 weeks of age)
Dosage:10 mg/kg
Administration:Oral administration; daily, for 21 days
Result:Inhibited tumor growth with GI (tumor volume growth inhibition)=47.66% and TGI (tumor weight growth inhibition)=62.39%.Exhibited no significant changes in behavior or body weight in mice.Had no obvious liver injury.
Animal Model:Male Sprague-Dawley rats (240±20 g)
Dosage:2 mg/kg (i.v.) and 20 mg/kg (p.o.) (Pharmacokinetic Analysis)
Administration:Intravenous injection and oral administration; once
Result:1.19Parameter2 mg/kg (i.v.)20 mg/kg (p.o.)
T1/2 (h)0.4611.77
Tmax (h)0.083/td>1.00
Cmax (ng/mL)20667.8
AUCo-t (h*ng/mL)110302
AUCo-∞ (h*ng/mL)115316
CL (L/h/kg)18.7
Vss(L/Kg)12.6
F (%)27.47
体外研究：
ZLMT-12 (compound 35; 500 nM; 72 h) has antiproliferative activity in cancer cells.ZLMT-12 (500 nM; 72 h) induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.
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