Afuresertib

• UNSPSC 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].

• Target Antigen:

  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

• 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 Weight:

  427.32

• 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):e100880Cancers (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.|Genes Dis. 2021 Aug 17;9(2):562-575.|Int J Cancer. 2020 Apr 1;146(7):1963-1978. |J Biol Chem. 2024 Jan 9:105641.|J Cell Biochem. 2024 Jun 11.|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.|Patent. US20230147129A1.

• Shipping Conditions:

  Blue Ice

• Clinical Information:

  Phase 3

• CAS Number:

  1047644-62-1