NTQ1062

Names

[ Name ]:
NTQ1062

Biological Activity

[Description]:

NTQ1062 (compound 22b) 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[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> PI3K/Akt/mTOR >> Akt

[Target]

Akt1:0.4 nM (IC50)

Akt2:6.3 nM (IC50)

Akt3:0.1 nM (IC50)

[In Vivo]

Pharmacokinetic Parameters of NTQ1062 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

[References]

[1]. Ma C, et al. Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors. J Med Chem. 2022 Jun 23;65(12):8144-8168.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₃₁ClN₆O₂

[ Molecular Weight ]:
483.01

Related Compounds

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