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Ipatasertib

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].

Product Specifications

CAS Number

[1001264-89-6]

Product Name Alternative

GDC-0068; RG7440

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

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

Purity

99.88

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 Formula

C24H32ClN5O2

Molecular Weight

458.00

Precautions

H302, H315, H319, H335

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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

Akt1; Akt2; Akt3

Citation 01

Biochem Biophys Res Commun. 2025 Jun 12:776:152203.|Biochem Pharmacol. 2020 Oct;180:114145.|Biomaterials. 2024 Mar: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.|bioRxiv. 2025 March 20.|bioRxiv. 2025 May 4:2025.04.29.651320.|Blood. 2023 Sep 14;142 (11) :973-988.|Br J Cancer. 2025 Sep 4.|Cancer Immunol Immunother. 2020 Nov;69 (11) :2259-2273.|Cancer Res. 2021 May 1;81 (9) :2470-2480.|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 Mol Med. 2025 Feb;17 (2) :336-364.|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 Biol Sci. 2025 Jan 27;21 (4) :1545-1565. |Int J Cancer. 2021 Sep 1;149 (5) :1137-1149.|Int J Hyperthermia. 2024 Feb 13;41 (1) :2310017.|J Cell Biochem. 2024 Aug;125 (8) :e30613.|Life Sci. 2020 Sep 1;256:117955.|Life Sci. 2021 Jul 15:277:119520.|Mol Cancer Ther. 2024 Oct 1;23 (10) :1404-1417.|Mol Oncol. 2024 Mar;18 (3) :726-742.|Mol Oncol. 2025 Jul 13.|Nat Cell Biol. 2025 Jan;27 (1) :73-86.|Nat Chem Biol. 2025 Aug;21 (8) :1194-1204.|Nat Commun. 2024 Dec 12;15 (1) :10476.|Nat Commun. 2025 Feb 25;16 (1) :1774.|Oncogene. 2025 Sep;44 (34) :3142-3148.|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.|Preprints. 2025 Nov 18.|Research Square Preprint. 2024 Nov 26.|Sci Adv. 2023 Mar 22;9 (12) :eadd5028.|Sci Adv. 2025 Apr 25;11 (17) :eads6385.|Sci Rep. 2025 Aug 17;15 (1) :30048.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Skelet Muscle. 2021 Mar 15;11 (1) :6.|SSRN. 2023 Jun 20.|Steroids. 2025 Sep 25:223:109692.|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.|Ren Fail. 2025 Dec;47 (1) :2580064.

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