NTQ1062 是一种有效且具有口服活性的Akt抑制剂，对 Akt1、Akt2 和 Akt3 的IC50分别为 0.4 nM、6.3 nM 和 0.1 nM。NTQ1062 诱导细胞凋亡 (apoptosis)，使细胞周期阻滞在 G0/G1 期。NTQ1062 对多种癌细胞具有抗增殖活性。NTQ1062 在 LNCap 异种移植瘤小鼠模型中显示出强大的抗肿瘤作用。
| 生物活性 | NTQ1062 is a potent and orally activeAktinhibitor withIC50s of 0.4 nM, 6.3 nM and 0.1 nM forAkt1,Akt2andAkt3, respectively. NTQ1062 induces cellapoptosisand arrests the cell cycle at G0/G1 phase. NTQ1062 exhibits antiproliferation activity against variouscancercells. NTQ1062 exhibits potent antitumor efficacy in LNCap xenograft mouse model[1]. |
| IC50& Target[1] | Akt1 0.4 nM (IC50) | Akt2 6.3 nM (IC50) | Akt3 0.1 nM (IC50) |
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体外研究
(In Vitro) | NTQ1062 (compound 22b) (0-4 μM; 72 h) has antiproliferative activity against various cancer cell lines[1].
NTQ1062 (2.5 μM; 72 h) induces LNCap cells apoptosis[1].
NTQ1062 (0.2 μM; 24 h) arrest LNCap cells at G0-G1 phase[1].
Cell Proliferation Assay[1] | Cell Line: | CAL-51, T-47D, COLO-704, TOV-21G, C-33A, and RL-95-2 cell lines | | Concentration: | 0-4μM | | Incubation Time: | 72 h | | Result: | Exhibited a strong inhibitory effect on the CAL-51, T-47D, COLO-704, TOV-21G, C-33A, and RL-95-2 cell lines with IC50s<300 nM. |
Apoptosis Analysis[1] | Cell Line: | LNCap cells | | Concentration: | 2.5 μM | | Incubation Time: | 72 h | | Result: | Caused the total number of apoptotic cells reaching 38.97%, while the control group was only 3.95%. |
Cell Cycle Analysis[1] | Cell Line: | LNCap cells | | Concentration: | 0.2 μM | | Incubation Time: | 24 h | | Result: | Caused 82.42% of cells in the G0-G1 phase, and decreased the populations of the S phase and G2-M phase. |
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体内研究
(In Vivo) | NTQ1062 (12.5, 25, and 50 mg/kg; PO; once daily for 18-21 days) exhibits tumor inhibitory effect[1].
NTQ1062 (5 mg/kg for IV, 10 mg/kg for IG; single dosage) exhibits good pharmacokinetic characteristics[1].
Pharmacokinetic Parameters of NTQ1062 (compound 22b) in male Sprague-Dawley rats[1].
| IV (5 mg/kg) | IG (10 mg/kg) | | Tmax(h) | | 2 | | t1/2(ng/mL) | 2.97 | 3.28 | | Cmax(ng/mL) | 1691 | 705 | | AUC0-t(ng/mL·h) | 1761 | 3877 | | AUC0-∞(ng/mL·h) | 1801 | 3891 | | 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 1×107cells/mL, 100 μL per mouse)[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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