AT7867
AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA (IC50=32 nM/17 nM/47 nM and 85 nM/20 nM, respectively).
Akt, also known as protein kinase B, is a serine/threonine-specific protein kinase that plays a key role in multiple cellular processes such as glucose metabolism, apoptosis, cell proliferation, transcription and cell migration.
AT7867 inhibited cell proliferation in multiple human cancer cell lines, it is most potent in inhibiting MES-SA uterine/MDA-MB-468/MCF-7 breast/HCT116/HT29 colon lines (IC50, 0.9–3 μM). AT7867 also inhibited GSK3β among each cell lines tested (IC50=2-4 μM). In U87MG human glioblastoma cells, AT7867 suppressed AKT signaling and induced apoptosis in a time and concentration-dependent manner. [1]
In athymic mice implanted with the PTEN-deficient U87MG human glioblastoma xenograft model, AT7867 treatment showed inhibition in phosphorylation of AKT/p70S6K downstream substrates and led to apoptosis. In PTEN-dificient xenograft models, AT7867 inhibited human tumor growth. [1]
Reference:
Grimshaw KM, Hunter LJ, Yap TA et al. AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth. Mol Cancer Ther. 2010 May;9(5):1100-10.
- 1. Chen-Xiao Liu, Su-Qin Hu, et al. "The effect of semen cuscutae flavonoid on Sertoli cells and blood-testis barrier in male infertility: integrating network pharmacology and experimental verification." Pharm Biol. 2023 Dec;61(1):986-999. PMID: 37386769
- 2. Yuchen Li, Yun Yuan, et al. "AT7867 Inhibits the Growth of Colorectal Cancer Stem-Like Cells and Stemness by Regulating the Stem Cell Maintenance Factor Ascl2 and Akt Signaling" Stem Cells International. 14 Feb 2023.
- 3. Ya-Hui Xu, Yue Li, et al. "Effect of Wuzi Yanzong Pills on Sertoli cells and blood–testis barrier in heat‐stressed rats based on Akt signalling pathway." Andrologia. 2021 Oct;53(9):e14169. PMID: 34197007
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 337.85 |
| Cas No. | 857531-00-1 |
| Formula | C20H20ClN3 |
| Solubility | ≥16.9 mg/mL in DMSO; ≥4.38 mg/mL in EtOH with ultrasonic; ≥45 mg/mL in H2O |
| Chemical Name | 4-(4-chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]piperidine |
| SDF | Download SDF |
| Canonical SMILES | C1CNCCC1(C2=CC=C(C=C2)C3=CNN=C3)C4=CC=C(C=C4)Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 values of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively | |||||
| Targets | Akt2 | PKA | Akt1 | Akt3 | p70 S6K | |
| IC50 | 17 nM | 20 nM | 32 nM | 47 nM | 85 nM | |
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Chemical structure
