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 |
| 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 |
| 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.
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