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Capivasertib (AZD5363) is a potentially first-in-class, orally effective pan-AKT inhibitor with strong inhibition against all three AKT isomers (AKT1/2/3) at an IC50 of 3 nM/8 nM/8 nM. It also showed similar inhibitory effect on P70S6K/PKA and low inhibitory activity on ROCK1/2.
Oxid Med Cell Longev. 2021 Jun 14;2021:6662225.
Impaired Autophagy Induced by oxLDL/ β 2GPI/anti- β 2GPI Complex through PI3K/AKT/mTOR and eNOS Signaling Pathways Contributes to Endothelial Cell Dysfunction
Capivasertib (AZD5363) purchased from AbMole
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Source | Oxid Med Cell Longev (2021). Figure 5. (Abmole Bioscience, USA) |
| Method | Cell Culture and Treatment | |
| Cell Lines | HUVECs and bEnd.3 cells | |
| Concentrations | 100 μM | |
| Incubation Time | 4 h | |
| Results | We found that LY294002, AZD5363, rapamycin, and L-NAME pretreatment could significantly upregulate the expression of LC3-II, while downregulating the expression of p62 compared with the oxLDL/β2GPI/anti-β2GPI complex alone group |
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Source | Cancer Biol Ther (2018). Figure 3. AZD5363 |
| Method | Western blot | |
| Cell Lines | HEK293T cells | |
| Concentrations | 250 mg/kg | |
| Incubation Time | 24 h | |
| Results | Proliferation of homozygous H2189Y mutant cells was significantly inhibited by the mTOR inhibitor everolimus (P =0.018), the PI3K inhibitor LY294002 (P D 0.016), and the AKT inhibitors AZD5363 (P = 0.009) and MK-2206 (P = 0.003). The PI3K inhibitor Wortmannin had no significant effect on proliferation in these five cell lines |
| Cell Experiment | |
|---|---|
| Cell lines | MCF7 (PIK3CA E545K mutant) and T47D (PI3KCA H1047R mutant) cells |
| Preparation method | Cells harvested and diluted to 1.0 × 10^4 cells/mL. Then, 100 μL was added to black 96 well plate for each cell line and incubated for an hour/overnight at 37 °C, 5% CO2. Next, 100 μL growth media was added to give the final plate volume of 200 μL. Compound was added from 10 mM capivasertib and 0.1 mM DMSO fulvestrant using an HP D300E dispenser. Cell confluence reads were taken every 8 h for 96 h at 37 °C, 5% CO2 using an Incucyte. |
| Concentrations | 10 mM |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | Female Athymic Nude Mice |
| Formulation | 10% DMSO+25% Kleptose+ddH20，pH 5 |
| Dosages | 130 mg/kg, 100 mg/kg or 65 mg/kg |
| Administration | Oral gavage |
| Molecular Weight | 428.92 |
| Formula | C21H25ClN6O2 |
| CAS Number | 1143532-39-1 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Akt Products |
|---|
| AT7867
AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase with an IC50 of 17 nM. |
| GSK690693
GSK690693 is a potent Akt inhibitor (Akt1 IC50 = 2 nM, Akt2 IC50 = 13 nM, Akt3 IC50 = 9 nM) which also inhibited the phosphorylation of the downstream target GSK3b in cells. |
| Perifosine
Perifosine is an orally active Akt inhibitor, the antiproliferative properties of Perifosine with an IC50 of 0.6–8.9 µM. |
| MK-2206 2HCl
MK-2206 is a novel allosteric inhibitor of Akt with IC50 values of 8 nM, 12 nM and 65 nM for Akt1, Akt2 and Akt3, respectively. |
| Ipatasertib
Ipatasertib (GDC-0068, RG7440) is a potent and selective, ATP-competitive Akt inhibitor with IC50 values of 5 to 18 nM. |
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