Afuresertib

• Description:

  Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively[1][2].

• Product Name Alternative:

  GSK2110183; LAE002

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  Akt; PKC; ROCK

• Type:

  Reference compound

• Related Pathways:

  Cell Cycle/DNA Damage; Cytoskeleton; Epigenetics; PI3K/Akt/mTOR; Stem Cell/Wnt; TGF-beta/Smad

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Afuresertib.html

• Concentration:

  10mM

• Purity:

  99.53

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=CC(F)=C3)CN

• Molecular Formula:

  C18H17Cl2FN4OS

• Molecular Weight:

  427.32

• Precautions:

  H302, H315, H319, H335

• References & Citations:

  [1]Yamaji M, et al. Novel ATP-competitive Akt inhibitor Afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6 (11) :2646-2659.|[2]Dumble M, et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9 (6) :e100880

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, protect from light, stored under nitrogen)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 3

• Isoform:

  Akt1; Akt2; Akt3; PKCβ; PKCη; PKCθ; ROCK

• Citation 01:

  Cancers (Basel) . 2022 May 19;14 (10) :2493.|Cell Syst. 2018 Apr 25;6 (4) :424-443.e7.|Cell. 2024 Feb 1;187 (3) :624-641.e23.|Cold Spring Harb Mol Case Stud. 2022 Jan 10;8 (1) :a006140.|Food Chem Toxicol. 2025 Oct:204:115628.|Genes Dis. 2021 Aug 17;9 (2) :562-575.|Int J Cancer. 2020 Apr 1;146 (7) :1963-1978.|J Biol Chem. 2024 Feb;300 (2) :105641.|J Cell Biochem. 2024 Aug;125 (8) :e30613.|J Physiol. 2017 Jul 1;595 (13) :4207-4225.|Methods Mol Biol. 2018:1711:351-398.|Molecules. 2019 Apr 1;24 (7) :1260.|Research Square Print. October 27th, 2022.|Sci Transl Med. 2021 Jan 27;13 (578) :eaba7308.|Theranostics. 2019 Jan 30;9 (4) :1096-1114.|Biomed Pharmacother. 2025 Nov:192:118707. |bioRxiv. 2025 Jun 16.|Patent. US20230147129A1.

• CAS Number:

  [1047644-62-1]