2. PI3K/Akt/mTOR
  3. Akt
  4. NTQ1062

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.

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NTQ1062 Chemical Structure

NTQ1062 Chemical Structure

CAS No. : 2459489-66-6

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NTQ1062 Related Antibodies

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Description

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[1].

IC50 & Target[1]

Akt1

0.4 nM (IC50)

Akt2

6.3 nM (IC50)

Akt3

0.1 nM (IC50)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NTQ1062 Related Antibodies

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.
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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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)[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.
Molecular Weight

483.01

Formula

C25H31ClN6O2
CAS No.
SMILES

CC(C)NC[C@H](C1=CC=C(C=C1)Cl)C(N2[C@@]3([H])[C@@](C3)([H])N(C4=C5C(NC=N4)=NC(C[C@H]5C)=O)CC2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NTQ1062 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NTQ10622459489-66-6NTQ 1062NTQ-1062AktPKBProtein kinase BanticancerantiproliferativeLNCapRL-95-2C-33ACOLO-704Inhibitorinhibitorinhibit

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