Afuresertib hydrochloride

SKU: orb1299415

Description

Afuresertib hydrochloride is a potent and selective pan-Akt kinase inhibitor, exhibiting Kis of 0.08, 2, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. It is widely used in preclinical research to investigate the PI3K/Akt signaling pathway in cancer, with applications in both in vitro cellular assays and in vivo xenograft models.

Research Area

Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1047645-82-8
• MW: 463.8
• Purity: 99.96%
• Formula: C₁₈H₁₈Cl₃FN₄OS
• SMILES: Cl.Cn1ncc(Cl)c1-c1cc(sc1Cl)C(=O)N[C@H](CN)Cc1cccc(F)c1
• Target: Akt,PKC,ROCK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.62 mM);DMSO:100 mg/mL (215.61 mM)

Bioactivity

• Target IC50:
  PKCη:210 nM|PKCθ:510 nM|Akt3:2.6 nM(Ki)|Akt1 E17K mutant:0.2 nM|ROCK:100 nM|PKCβI:430 nM|Akt2:2 nM(Ki)|Akt1:0.08 nM(Ki)
• In Vitro:
  Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity. Furthermore, afuresertib significantly enhanced cisplatin-induced cytotoxicity.Afuresertib modulated the expression E2F1 and MYC, which are associated with fibroblast core serum response. Suggest that afuresertib is a useful anticancer drug for treating patients with MPM.
• Cell Research:
  Cell confluence proliferation assay was performed using Incucyte ZOOM Live‐Cell Imaging System. Briefly, ACC‐MESO‐4 and MSTO‐211H cells were seeded in 12‐well plates (cell density, 1 × 104 cells/well) and were incubated for 24 h at 37°C. Then, the cells were incubated with 0, 2, 5, or 10 μmol/L afuresertib. During treatment, cell growth was monitored by recording phase images using the IncuCyte ZOOM Live‐Cell Imaging System (magnification, ×100).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, GSK2110183, GSK-2110183, GSK 2110183, Inhibitor, Akt, Afuresertib, Afuresertib Hydrochloride, Afuresertib hydrochloride, Protein kinase C, Protein kinase B, Rho-kinase, Rho-associated kinase, Rho-associated protein kinase, ROK, ROCK, PKB, PKC

Compound Identifiers

PubChem CID

46843056