Ipatasertib tosylate
Based on 69 publication(s) in Google Scholar
Ipatasertib (GDC-0068) tosylate 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 tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models.
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- CAS No.: 1491138-24-9
- Formule: C31H40ClN5O5S
- Masse moléculaire:630.20
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Ipatasertib tosylate
More- Cell Metab. 2021 Nov 2;33(11):2247-2259.e6. [Abstract]
- Blood. 2023 Sep 14;142(11):973-988. [Abstract]
- Nat Cell Biol. 2025 Jan;27(1):73-86. [Abstract]
- Cancer Res. 2021 May 1;81(9):2470-2480. [Abstract]
- Nat Commun. 2025 Feb 25;16(1):1774. [Abstract]
- Nat Commun. 2024 Dec 12;15(1):10476. [Abstract]
- Mol Cell. 2020 Sep 17;79(6):1008-1023.e4. [Abstract]
- Mol Cell. 2019 Jan 3;73(1):22-35.e6. [Abstract]
- Nat Chem Biol. 2025 Aug;21(8):1194-1204. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Sci Adv. 2025 Apr 25;11(17):eads6385. [Abstract]
- Sci Adv. 2023 Mar 22;9(12):eadd5028. [Abstract]
- Biomaterials. 2024 Mar:305:122462. [Abstract]
- Small. 2026 May;22(30):e73336. [Abstract]
- Int J Biol Sci. 2025 Jan 27;21(4):1545-1565. [Abstract]
- Oncogene. 2025 Sep;44(34):3142-3148. [Abstract]
- Int J Biol Macromol. 2026 May:362:152113. [Abstract]
- Haematologica. 2020 Mar;105(3):661-673. [Abstract]
- EMBO Mol Med. 2025 Feb;17(2):336-364. [Abstract]
- Br J Cancer. 2025 Sep 4. [Abstract]
- Aging Cell. 2026 Jul;25(7):e70623.
- Cell Rep. 2026 Jul 28;45(7):117694.
- Cell Rep. 2021 Feb 16;34(7):108744. [Abstract]
- Food Sci Hum Wellness. 2026 Jun 24.
- Mol Cancer Ther. 2024 Oct 1;23(10):1404-1417. [Abstract]
- Biochem Pharmacol. 2020 Oct:180:114145. [Abstract]
- Life Sci. 2021 Jul 15:277:119520. [Abstract]
- Life Sci. 2020 Sep 1:256:117955. [Abstract]
- Oncoimmunology. 2018 Aug 6;7(10):e1488565. [Abstract]
- EMBO Rep. 2020 Mar 4;21(3):e49129. [Abstract]
- Cancer Immunol Immunother. 2020 Nov;69(11):2259-2273. [Abstract]
- Sci Rep. 2025 Aug 17;15(1):30048. [Abstract]
- Int J Cancer. 2021 Sep 1;149(5):1137-1149. [Abstract]
- Cancers (Basel). 2023 Nov 14;15(22):5407. [Abstract]
- Neuropharmacology. 2026 Nov 1:298:111050. [Abstract]
- Oncol Rep. 2018 Aug;40(2):635-646. [Abstract]
- Mol Oncol. 2025 Jul 13. [Abstract]
- Mol Oncol. 2024 Mar;18(3):726-742. [Abstract]
- Skelet Muscle. 2021 Mar 15;11(1):6. [Abstract]
- Ren Fail. 2025 Dec;47(1):2580064. [Abstract]
- Front Oncol. 2021 Nov 24:11:766298. [Abstract]
- J Cell Biochem. 2024 Aug;125(8):e30613. [Abstract]
- Int J Hyperthermia. 2024 Feb 13;41(1):2310017. [Abstract]
- Steroids. 2025 Nov:223:109692. [Abstract]
- Biochem Biophys Res Commun. 2025 Aug 30:776:152203. [Abstract]
- Onco Targets Ther. 2020 Aug 18:13:8197-8208. [Abstract]
- Biomed Chromatogr. 2020 Oct;34(10):e4920. [Abstract]
- Biomed Chromatogr. 2020 Oct;34(10):e4923. [Abstract]
- Res Sq. 2026 Jun 15:rs.3.rs-9941989. [Abstract]
- J Mol Liq. 2026 May 23;457:129686.
- bioRxiv. 2026 Apr 9.
- Res Sq. 2026 Jan 15.
- Technical University of Dresden. 2025.
- Universite du Quebec. 2025.
- Preprints. 2025 Nov 18.
- bioRxiv. 2025 May 4:2025.04.29.651320. [Abstract]
- bioRxiv. 2025 March 20.
- Research Square Preprint. 2024 Nov 26.
- bioRxiv. 2024 August 26.
- bioRxiv. 2024 September 07.
- bioRxiv. 2024 August 18.
- bioRxiv. 2024 Jan 16.
- SSRN. 2023 Jun 20.
- Patent. US20220313694A1.
- Cold Spring Harb Mol Case Stud. 2022 Jan 10;8(1):a006140. [Abstract]
- Oxid Med Cell Longev. 2021 Jan 12:2021:3010548. [Abstract]
- Elife. 2020 Dec 7:9:e61405. [Abstract]
- Radboud University Nijmegen. 2019 Oct.
- Oncotarget. 2016 May 17;7(20):29131-42. [Abstract]
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Cell Proliferation/Viability Assay
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WB
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WB
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WB
Activité biologique
Description
IC50 & Target
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Akt1 5 nM (IC50) |
Akt2 18 nM (IC50) |
Akt3 8 nM (IC50) |
PKA 3100 nM (IC50) |
In Vitro
Ipatasertib tosylate (10 µM; 12, 24 h) suppresses colon cancer cell proliferation by p53 irrespectively activating PUMA in vitro[1].
Ipatasertib tosylate (1, 5, 10, 20 μM; 24 h/10 μM; 3, 6, 12, 24 h) up-regulates the expression level of PUMA in a concentration and time dependent manner in HCT116 cells[1].
Ipatasertib tosylate increases the mRNA level of PUMA in HCT116 WT, p53−/−, and DLD1 (p53 mutant) cells[1].
Ipatasertib tosylate (10 µM; 24 h) induces apoptosis through PUMA/Bax pathway in HCT116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 WT, p53−/−, and DLD1 (p53 mutant) cells
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Concentration:10 µM
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Incubation Time:12, 24 h
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Result:Decreased all the three cell lines viability.
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Cell Line:HCT116 cells
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Concentration:10 µM
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Incubation Time:24 h
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Result:Induced apoptosis through PUMA/Bax pathway.
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Cell Line:HCT116 WT, p53−/−, and DLD1 (p53 mutant) cells
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Concentration:1, 5, 10, 20 μM for 24 h/10 μM for 3, 6, 12, 24 h
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Incubation Time:24 h; 3, 6, 12, 24 h
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Result:Increased the level of PUMA in a concentration and time dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116 WT and PUMA−/− cells xenograft nude mice model[1].
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Dosage:30 mg/kg
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Administration:Oral gavage; single daily for 15 consecutive days.
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Result:Inhibited growth of tumors in a PUMA-dependent manner.
Chemical Information
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CAS No. 1491138-24-9
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Masse moléculaire 630.20
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Formule C31H40ClN5O5S
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SMILES
O=S(O)(C1=CC=C(C=C1)C)=O.ClC2=CC=C([C@@H](CNC(C)C)C(N3CCN(C4=C([C@H](C)C[C@H]5O)C5=NC=N4)CC3)=O)C=C2
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Synonyms
GDC-0068 tosylate; RG7440 tosylate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (69)
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Journal Impact Factor
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Most Recent
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Cell Metab
2021 Nov 2;33(11):2247-2259.e6. PMID: 34731655 -
Blood
DLBCL associated NOTCH2 mutations escape ubiquitin-dependent degradation and promote chemo-resistance. [Abstract]2023 Sep 14;142(11):973-988. PMID: 37235754 -
Nat Cell Biol
Chromosome mis-segregation triggers cell cycle arrest through a mechanosensitive nuclear envelope checkpoint. [Abstract]2025 Jan;27(1):73-86. PMID: 39779939 -
Cancer Res
Genomic Alterations in PIK3CA-Mutated Breast Cancer Result in mTORC1 Activation and Limit the Sensitivity to PI3Kα Inhibitors. [Abstract]2021 May 1;81(9):2470-2480. PMID: 33685991 -
Nat Commun
Attenuated growth factor signaling during cell death initiation sensitizes membranes towards peroxidation. [Abstract]2025 Feb 25;16(1):1774. PMID: 40000627
Ipatasertib tosylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 25;16(1):1774. [Abstract]
Viable cell numbers and PUFA-PC ratio after treatment with LY294002 (iPI3K, 10 µM), picropodophyllin (iRTK, 10 µM), ipatasertib (iAkt, 10 µM), or fatostatin (iSREBP1, 20 µM) for 48 h.
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Nat Commun
An actin bracket-induced elastoplastic transition determines epithelial folding irreversibility. [Abstract]2024 Dec 12;15(1):10476. PMID: 39668169 -
Mol Cell
DNA Damage Promotes TMPRSS2-ERG Oncoprotein Destruction and Prostate Cancer Suppression via Signaling Converged by GSK3β and WEE1. [Abstract]2020 Sep 17;79(6):1008-1023.e4. PMID: 32871104 -
Mol Cell
Phosphorylated RB Promotes Cancer Immunity by Inhibiting NF-κB Activation and PD-L1 Expression. [Abstract]2019 Jan 3;73(1):22-35.e6. PMID: 30527665 -
Nat Chem Biol
2025 Aug;21(8):1194-1204. PMID: 39934397 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Sci Adv
2025 Apr 25;11(17):eads6385. PMID: 40279411 -
Sci Adv
Breast tumors interfere with endothelial TRAIL at the premetastatic niche to promote cancer cell seeding. [Abstract]2023 Mar 22;9(12):eadd5028. PMID: 36947620 -
Biomaterials
FAK-p38 signaling serves as a potential target for reverting matrix stiffness-modulated liver sinusoidal endothelial cell defenestration. [Abstract]2024 Mar:305:122462. PMID: 38171118 -
Small
High-Throughput Single-Cell Biochip System for Functional Interrogation of Protein Interactions in Living Cells. [Abstract]2026 May;22(30):e73336. PMID: 41944250 -
Int J Biol Sci
High-dose Ascorbate Exhibits Anti-proliferative and Anti-invasive Effects Dependent on PTEN/AKT/mTOR Pathway in Endometrial Cancer in vitro and in vivo. [Abstract]2025 Jan 27;21(4):1545-1565. PMID: 39990670 -
Oncogene
Identification of RAPGEF3 as the therapeutic vulnerability of basal-subtype lung squamous cell carcinoma. [Abstract]2025 Sep;44(34):3142-3148. PMID: 40781157 -
Int J Biol Macromol
Acetylation of GPRC5A at Lys348 facilitates cisplatin resistance and promotes the recurrence and poor prognosis in ovarian cancer. [Abstract]2026 May:362:152113. PMID: 42009151 -
Haematologica
2020 Mar;105(3):661-673. PMID: 31289202 -
EMBO Mol Med
2025 Feb;17(2):336-364. PMID: 39748059 -
Br J Cancer
Inhibition of YB-1 phosphorylation enhances cisplatin activity and disrupts cell division in pleural mesothelioma. [Abstract]2025 Sep 4. PMID: 40908296 -
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Cell Rep
An acetyl-histone vulnerability in PI3K/AKT inhibition-resistant cancers is targetable by both BET and HDAC inhibitors. [Abstract]2021 Feb 16;34(7):108744. PMID: 33596421 -
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Mol Cancer Ther
AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. [Abstract]2024 Oct 1;23(10):1404-1417. PMID: 38894678 -
Biochem Pharmacol
20(S)-ginsenoside Rg3 promotes myoblast differentiation and protects against myotube atrophy via regulation of the Akt/mTOR/FoxO3 pathway. [Abstract]2020 Oct:180:114145. PMID: 32653593
Ipatasertib tosylate purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2020 Oct:180:114145. [Abstract]
C2C12 myoblasts were pre-incubated with 2.5 μM GDC-0068 for 30 min then treated with 0.2 μM S-Rg3. After incubation with S-Rg3 for 72 h and 24 h, Western blotting is used to detect levels of Myf5 and myogenin in C2C12 myoblasts after incubation of cells with S-Rg3 for 120 h. GDC-0068 inhibits S-Rg3-activated phosphorylation of Akt and mTOR in C2C12 myoblasts.
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Life Sci
Early-senescent bone marrow mesenchymal stem cells promote C2C12 cell myogenic differentiation by preventing the nuclear translocation of FOXO3. [Abstract]2021 Jul 15:277:119520. PMID: 33887345 -
Life Sci
2020 Sep 1:256:117955. PMID: 32534038 -
Oncoimmunology
Ex vivo AKT-inhibition facilitates generation of polyfunctional stem cell memory-like CD8+ T cells for adoptive immunotherapy. [Abstract]2018 Aug 6;7(10):e1488565. PMID: 30288356 -
EMBO Rep
2020 Mar 4;21(3):e49129. PMID: 32030864 -
Cancer Immunol Immunother
Cell composition and expansion strategy can reduce the beneficial effect of AKT-inhibition on functionality of CD8+ T cells. [Abstract]2020 Nov;69(11):2259-2273. PMID: 32504246 -
Sci Rep
Dendrobium officinale Kimura & Migo polysaccharide ameliorates skin photoaging by promoting angiogenesis. [Abstract]2025 Aug 17;15(1):30048. PMID: 40820014 -
Int J Cancer
Effects of Metformin on the virus/host cell crosstalk in human papillomavirus-positive cancer cells. [Abstract]2021 Sep 1;149(5):1137-1149. PMID: 33844847 -
Cancers (Basel)
Oleic Acid Exhibits Anti-Proliferative and Anti-Invasive Activities via the PTEN/AKT/mTOR Pathway in Endometrial Cancer. [Abstract]2023 Nov 14;15(22):5407. PMID: 38001668 -
Neuropharmacology
Hypericin alleviates high glucose-induced ferroptosis in cultured rat satellite glial cells via targeting P2X7R to activate the Akt/GSK3β/Nrf2 axis. [Abstract]2026 Nov 1:298:111050. PMID: 42214457 -
Oncol Rep
Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues. [Abstract]2018 Aug;40(2):635-646. PMID: 29917168 -
Mol Oncol
Olaparib synergy screen reveals Exemestane induces replication stress in triple-negative breast cancer. [Abstract]2025 Jul 13. PMID: 40652528 -
Mol Oncol
Dual targeting of the androgen receptor and PI3K/AKT/mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis. [Abstract]2024 Mar;18(3):726-742. PMID: 38225213 -
Skelet Muscle
MiR-1290 promotes myoblast differentiation and protects against myotube atrophy via Akt/p70/FoxO3 pathway regulation. [Abstract]2021 Mar 15;11(1):6. PMID: 33722298
Ipatasertib tosylate purchased from MedChemExpress. Usage Cited in: Skelet Muscle. 2021 Mar 15;11(1):6. [Abstract]
The western blot analysis and quantification of phosphorylated and all forms of AKT and P70, MyoG, and MyoD, after transfecting miR-1290/miR-NC with or without GDC0068. GDC-0068 inhibits miR-1290-activated phosphorylation of AKT and P70 in C2C12 myoblasts.
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Ren Fail
A multi-omics landscape of programmed cell death in acetaminophen-induced acute kidney injury. [Abstract]2025 Dec;47(1):2580064. PMID: 41249093 -
Front Oncol
Zotatifin, an eIF4A-Selective Inhibitor, Blocks Tumor Growth in Receptor Tyrosine Kinase Driven Tumors. [Abstract]2021 Nov 24:11:766298. PMID: 34900714
Ipatasertib tosylate purchased from MedChemExpress. Usage Cited in: Front Oncol. 2021 Nov 24:11:766298. [Abstract]
Ipatasertib (0.625, 1.25, 5 µM; 24 h) increases the phosphorylation of AKT in MFM-223 FGFR2amp cells.
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J Cell Biochem
2024 Aug;125(8):e30613. PMID: 38860522 -
Int J Hyperthermia
Impacts of hyperthermic chemotherapeutic agent on cytotoxicity, chemoresistance-related proteins and PD-L1 expression in human gastric cancer cells. [Abstract]2024 Feb 13;41(1):2310017. PMID: 38350654 -
Steroids
Kobochromone A, a polyphenol in Carex kobomugi, suppresses androgen signaling induced by 11-oxygenated androgens and enhances the efficacy of AKT inhibitors in triple-negative breast cancer cells. [Abstract]2025 Nov:223:109692. PMID: 41015102 -
Biochem Biophys Res Commun
Loss of DNA replication fork protection by TIMELESS degradation supports oncogene-induced senescence. [Abstract]2025 Aug 30:776:152203. PMID: 40517672 -
Onco Targets Ther
Inhibition of PI3K-AKT Signaling Blocks PGE2-Induced COX-2 Expression in Lung Adenocarcinoma. [Abstract]2020 Aug 18:13:8197-8208. PMID: 32904445 -
Biomed Chromatogr
A validated LC-MS/MS method for the quantification of capivasertib in dog plasma: Application to its pharmacokinetics study. [Abstract]2020 Oct;34(10):e4920. PMID: 32537750 -
Biomed Chromatogr
2020 Oct;34(10):e4923. PMID: 32558944 -
Res Sq
ERG function in prostate cells is regulated by distinct positive feedback loops depending on AKT signaling status. [Abstract]2026 Jun 15:rs.3.rs-9941989. PMID: 42370241 -
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bioRxiv
2025 May 4:2025.04.29.651320. PMID: 40654780 -
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Cold Spring Harb Mol Case Stud
Functional impact and targetability of PI3KCA, GNAS, and PTEN mutations in a spindle cell rhabdomyosarcoma with MYOD1 L122R mutation. [Abstract]2022 Jan 10;8(1):a006140. PMID: 35012940 -
Oxid Med Cell Longev
2021 Jan 12:2021:3010548. PMID: 33505580 -
Elife
2020 Dec 7:9:e61405. PMID: 33284104 -
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Oncotarget
Dual inhibition of AKT/FLT3-ITD by A674563 overcomes FLT3 ligand-induced drug resistance in FLT3-ITD positive AML. [Abstract]2016 May 17;7(20):29131-42. PMID: 27074558
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)