产品
编 号：F752959
分子式：C25H31ClN6O2
分子量：483.01
分子式：C25H31ClN6O2
分子量：483.01
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CAS No: 2459489-66-6
产品详情
生物活性：
NTQ1062 is a potent and orally active Akt inhibitor with IC50s of 0.4 nM, 6.3 nM and 0.1 nM for Akt1, Akt2 and Akt3, respectively. NTQ1062 induces cell apoptosis and arrests the cell cycle at G0/G1 phase. NTQ1062 exhibits antiproliferation activity against various cancer cells. NTQ1062 exhibits potent antitumor efficacy in LNCap xenograft mouse model.
体内研究：
NTQ1062 (12.5, 25, and 50 mg/kg; PO; once daily for 18-21 days) exhibits tumor inhibitory effect.NTQ1062 (5 mg/kg for IV, 10 mg/kg for IG; single dosage) exhibits good pharmacokinetic characteristics.Pharmacokinetic Parameters of NTQ1062 (compound 22b) in male Sprague-Dawley rats.IV (5 mg/kg) IG (10 mg/kg)
Tmax (h)2
t1/2 (ng/mL)2.973.28
Cmax (ng/mL)1691705
AUC0-t (ng/mL·h)17613877
AUC0-∞ (ng/mL·h)18013891
VSS (L/kg)7.76
F (%)110
Animal Model:Male NCG mice (24-30 g; inoculated subcutaneously with LNCap in the right hind flank at the density of 1×107 cells/mL, 100 μL per mouse)
Dosage:12.5, 25, and 50 mg/kg
Administration:PO; once daily for 18-21 days
Result:Exhibited a dose-dependent tumor suppressive effect, with TGIs of 58.4%, 84.1%, and 95.5% at 12.5, 25, and 50 mg/kg, respectively.
体外研究：
NTQ1062 (compound 22b) (0-4 μM; 72 h) has antiproliferative activity against various cancer cell lines.NTQ1062 (2.5 μM; 72 h) induces LNCap cells apoptosis.NTQ1062 (0.2 μM; 24 h) arrest LNCap cells at G0-G1 phase.
NTQ1062 is a potent and orally active Akt inhibitor with IC50s of 0.4 nM, 6.3 nM and 0.1 nM for Akt1, Akt2 and Akt3, respectively. NTQ1062 induces cell apoptosis and arrests the cell cycle at G0/G1 phase. NTQ1062 exhibits antiproliferation activity against various cancer cells. NTQ1062 exhibits potent antitumor efficacy in LNCap xenograft mouse model.
体内研究：
NTQ1062 (12.5, 25, and 50 mg/kg; PO; once daily for 18-21 days) exhibits tumor inhibitory effect.NTQ1062 (5 mg/kg for IV, 10 mg/kg for IG; single dosage) exhibits good pharmacokinetic characteristics.Pharmacokinetic Parameters of NTQ1062 (compound 22b) in male Sprague-Dawley rats.IV (5 mg/kg) IG (10 mg/kg)
Tmax (h)2
t1/2 (ng/mL)2.973.28
Cmax (ng/mL)1691705
AUC0-t (ng/mL·h)17613877
AUC0-∞ (ng/mL·h)18013891
VSS (L/kg)7.76
F (%)110
Animal Model:Male NCG mice (24-30 g; inoculated subcutaneously with LNCap in the right hind flank at the density of 1×107 cells/mL, 100 μL per mouse)
Dosage:12.5, 25, and 50 mg/kg
Administration:PO; once daily for 18-21 days
Result:Exhibited a dose-dependent tumor suppressive effect, with TGIs of 58.4%, 84.1%, and 95.5% at 12.5, 25, and 50 mg/kg, respectively.
体外研究：
NTQ1062 (compound 22b) (0-4 μM; 72 h) has antiproliferative activity against various cancer cell lines.NTQ1062 (2.5 μM; 72 h) induces LNCap cells apoptosis.NTQ1062 (0.2 μM; 24 h) arrest LNCap cells at G0-G1 phase.
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