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Afuresertib hydrochloride

Cat. No. M9024
Afuresertib hydrochloride Structure
Synonym:

GSK2110183B; Afuresertib HCl

Size Price Availability
10mg USD 165 4-7 Days
50mg USD 520 4-7 Days
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Quality Control
  • Current batch:
  • Purity >97%
  • COA
  • MSDS
Biological Activity

Afuresertib HCl binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response.

Protocol
Cell Experiment
Cell lines MPM cells
Preparation method MPM cells are seeded in 96-well plates (cell density, 2.5×103 cells/well) and are incubated for 24 h at 37°C. Next, the cells are incubated in a medium containing indicated concentrations of Akt inhibitors (e.g., Afuresertib ; 50, 20, 10, 5, 2, 1, 0.5, 0.2, 0.1, and 0.01 μM) for 72 h. Next, MTT solution is added to each well, and the cells are incubated for 4 h. Finally, the cells are incubated overnight with lysis buffer (10% SDS in 0.01 mol/L hydrogen chloride). Absorbance is measured at 550 nm using SpectraMAX M5 spectrophotometer.
Concentrations 50, 20, 10, 5, 2, 1, 0.5, 0.2, 0.1, and 0.01 μM
Incubation time 72 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 463.78
Formula C18H18Cl3FN4OS
CAS Number 1047645-82-8
Purity >97%
Solubility DMSO: ≥ 40 mg/mL
Storage at -20°C
References

Novel ATP-competitive Akt inhibitor afuresertib suppresses the proliferation of malignant pleural mesothelioma cells.
Yamaji M, et al. Cancer Med. 2017 Nov;6(11):2646-2659. PMID: 28960945.

The novel AKT inhibitor afuresertib shows favorable safety, pharmacokinetics, and clinical activity in multiple myeloma.
Spencer A, et al. Blood. 2014 Oct 2;124(14):2190-5. PMID: 25075128.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Afuresertib hydrochloride, GSK2110183B; Afuresertib HCl supplier, Akt, inhibitors

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