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NTQ1062

Cat. No. M21054
NTQ1062  Structure
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Biological Activity

NTQ1062 is an oral ATP-competitive Akt inhibitor being developed for cancer. The IC50 of Akt1, Akt2 and Akt3 were 0.4 nM, 6.3 nM and 0.1 nM, respectively. Apoptosis induced by NTQ1062 resulted in cell cycle arrest at G0/G1 phase. NTQ1062 has anti-proliferation activity against a variety of cancer cells. NTQ1062 showed potent antitumor effects in the LNCap xenograft tumor mouse model.

Chemical Information
Molecular Weight 483.01
Formula C25H31ClN6O2
CAS Number 2459489-66-6
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Changyou Ma, et al. J Med Chem. Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors

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Keywords: NTQ1062 supplier, Akt, inhibitors, activators


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