Ipatasertib

Ipatasertib

• CAS Number: 1001264-89-6
• UNSPSC Description: Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models[1][2].
• Target Antigen: Akt; Apoptosis; Organoid
• Type: Reference compound
• Related Pathways: Apoptosis;PI3K/Akt/mTOR;Stem Cell/Wnt
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/GDC-0068.html
• Solubility: DMSO : 100 mg/mL (ultrasonic)|H2O : 3.57 mg/mL (ultrasonic;warming;heat to 60°C)
• Smiles: ClC1=CC=C([C@@H](CNC(C)C)C(N2CCN(C3=C([C@H](C)C[C@H]4O)C4=NC=N3)CC2)=O)C=C1
• Molecular Weight: 458.00
• References & Citations: [1]Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27.|[2]Sun L, et al. Ipatasertib, a novel Akt inhibitor, induces transcription factor FoxO3a and NF-κB directly regulates PUMA-dependent apoptosis. Cell Death Dis. 2018 Sep 5;9(9):911.Biochem Pharmacol. 2020 Oct;180:114145.|Biomaterials. 2024 Jan 1:305:122462.|Biomed Chromatogr. 2020 Oct;34(10):e4920.|Biomed Chromatogr. 2020 Oct;34(10):e4923.|bioRxiv. 2024 August 18.|bioRxiv. 2024 August 26.|bioRxiv. 2024 Jan 16.|bioRxiv. 2024 September 07.|Blood. 2023 May 26;blood.2022018752.|Cancer Immunol Immunother. 2020 Nov;69(11):2259-2273.|Cancer Res. 2021 Mar 8;canres.3232.2020.|Cancers (Basel). 2023 Nov 14, 15(22), 5407.|Cell Metab. 2021 Nov 2;33(11):2247-2259.e6.|Cold Spring Harb Mol Case Stud. 2022 Jan 10;8(1):a006140.|Department of Laboratory Medicine, Laboratory of Hematology of the Radboudumc and Radboud Institute for Molecular Life Sciences in Nijmegen, The Netherlands.2019 Oct.|Elife. 2020 Dec 7;9:e61405.|EMBO Rep. 2020 Mar 4;21(3):e49129.|Front Oncol. 2021 Nov 24:11:766298.|Haematologica. 2020 Mar;105(3):661-673.|Harvard Medical School LINCS LIBRARY|Int J Cancer. 2021 Apr 12.|Int J Hyperthermia. 2024 Feb 13;41(1):2310017.|J Cell Biochem. 2024 Jun 11.|Life Sci. 2020 Sep 1;256:117955.|Life Sci. 2021 Apr 19;277:119520.|Mol Cancer Ther. 2024 Jun 19.|Mol Oncol. 2024 Jan 15.|Oncoimmunology. 2018 Aug 6;7(10):e1488565. |Oncol Rep. 2018 Aug;40(2):635-646. |Oncotarget. 2016 May 17;7(20):29131-42. |Oncotargets Ther. 2020 Aug 18;13:8197-8208.|Oxid Med Cell Longev. 2021 Jan 12;2021:3010548.|Patent. US20220313694A1.|Research Square Preprint. 2024 Nov 26.|Sci Adv. 2023 Mar 22;9(12):eadd5028.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Skelet Muscle. 2021 Mar 15;11(1):6.|SSRN. 2023 Jun 20.|Cell Rep. 2021 Feb 16;34(7):108744.|Mol Cell. 2020 Sep 17;79(6):1008-1023.e4.|Mol Cell. 2019 Jan 3;73(1):22-35.e6.
• Shipping Conditions: Room Temperature
• Clinical Information: Phase 3