Ipatasertib
Based on 63 publication(s) in Google Scholar
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.74%
- CAS No.: 1001264-89-6
- Formule: C24H32ClN5O2
- Masse moléculaire:458.00
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Ipatasertib
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]
- Mol Cell. 2020 Sep 17;79(6):1008-1023.e4. [Abstract]
- Mol Cell. 2019 Jan 3;73(1):22-35.e6. [Abstract]
- Nat Commun. 2025 Feb 25;16(1):1774. [Abstract]
- Nat Commun. 2024 Dec 12;15(1):10476. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Nat Chem Biol. 2025 Aug;21(8):1194-1204. [Abstract]
- Biomaterials. 2024 Mar:305:122462. [Abstract]
- Sci Adv. 2025 Apr 25;11(17):eads6385. [Abstract]
- Sci Adv. 2023 Mar 22;9(12):eadd5028. [Abstract]
- Int J Biol Sci. 2025 Jan 27;21(4):1545-1565. [Abstract]
- EMBO Mol Med. 2025 Feb;17(2):336-364. [Abstract]
- Haematologica. 2020 Mar;105(3):661-673. [Abstract]
- Oncogene. 2025 Sep;44(34):3142-3148. [Abstract]
- Cell Rep. 2021 Feb 16;34(7):108744. [Abstract]
- Br J Cancer. 2025 Sep 4. [Abstract]
- Elife. 2020 Dec 7;9:e61405. [Abstract]
- Oncoimmunology. 2018 Aug 6;7(10):e1488565. [Abstract]
- EMBO Rep. 2020 Mar 4;21(3):e49129. [Abstract]
- Biochem Pharmacol. 2020 Oct;180:114145. [Abstract]
- Mol Cancer Ther. 2024 Oct 1;23(10):1404-1417. [Abstract]
- J Mol Liq. 2026 May 23;457:129686.
- Life Sci. 2021 Jul 15:277:119520. [Abstract]
- Cancer Immunol Immunother. 2020 Nov;69(11):2259-2273. [Abstract]
- Life Sci. 2020 Sep 1;256:117955. [Abstract]
- Int J Cancer. 2021 Sep 1;149(5):1137-1149. [Abstract]
- Mol Oncol. 2025 Jul 13. [Abstract]
- Mol Oncol. 2024 Mar;18(3):726-742. [Abstract]
- Cancers (Basel). 2023 Nov 14;15(22):5407. [Abstract]
- Skelet Muscle. 2021 Mar 15;11(1):6. [Abstract]
- Sci Rep. 2025 Aug 17;15(1):30048. [Abstract]
- Oncol Rep. 2018 Aug;40(2):635-646. [Abstract]
- Front Oncol. 2021 Nov 24:11:766298. [Abstract]
- Ren Fail. 2025 Dec;47(1):2580064. [Abstract]
- Int J Hyperthermia. 2024 Feb 13;41(1):2310017. [Abstract]
- J Cell Biochem. 2024 Aug;125(8):e30613. [Abstract]
- Oncotargets Ther. 2020 Aug 18;13:8197-8208. [Abstract]
- Steroids. 2025 Sep 25:223:109692. [Abstract]
- Biochem Biophys Res Commun. 2025 Jun 12:776:152203. [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]
- 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.
- bioRxiv. 2024 August 26.
- Research Square Preprint. 2024 Nov 26.
- bioRxiv. 2024 August 18.
- bioRxiv. 2024 September 07.
- 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]
- 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
|
Akt1 5 nM (IC50) |
Akt3 8 nM (IC50) |
Akt2 18 nM (IC50) |
PKA 3100 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| AN3-CA | EC50 |
925 nM
Compound: Ipatasertib
|
Antiproliferative activity against human AN3-CA cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
Antiproliferative activity against human AN3-CA cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
|
[PMID: 30996949] |
| BT-474 | EC50 |
2371 nM
Compound: Ipatasertib
|
Antiproliferative activity against human BT-474 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
Antiproliferative activity against human BT-474 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
|
[PMID: 30996949] |
| BT-474 | GI50 |
0.3 μM
Compound: GDC-0068
|
Antiproliferative activity against human BT-474 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
Antiproliferative activity against human BT-474 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
|
[PMID: 34855399] |
| C-33-A | IC50 |
725.97 nM
Compound: GDC-0068
|
Antiproliferative activity against human C-33-A habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
Antiproliferative activity against human C-33-A habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
|
[PMID: 35679512] |
| CAL-51 | IC50 |
265.2 nM
Compound: GDC-0068
|
Antiproliferative activity against human CAL-51 habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
Antiproliferative activity against human CAL-51 habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
|
[PMID: 35679512] |
| Hep 3B2 | IC50 |
389 μM
Compound: GDC-0068
|
Cytotoxicity against human Hep3B cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human Hep3B cells assessed as reduction in cell viability by MTT assay
|
[PMID: 32007668] |
| HepG2 | IC50 |
0.268 μM
Compound: GDC-0068
|
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
|
[PMID: 32007668] |
| Huh-7 | IC50 |
0.167 μM
Compound: GDC-0068
|
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by MTT assay
|
[PMID: 32007668] |
| KU-19-19 | EC50 |
24037 nM
Compound: Ipatasertib
|
Antiproliferative activity against human KU-19-19 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
Antiproliferative activity against human KU-19-19 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
|
[PMID: 30996949] |
| LNCaP | IC50 |
157 nM
Compound: 28, GDC-0068
|
Inhibition of Akt1 in human LNCAP cells assessed as phosphorylation of PRAS40 at Thr246 after 1.5 hrs
Inhibition of Akt1 in human LNCAP cells assessed as phosphorylation of PRAS40 at Thr246 after 1.5 hrs
|
[PMID: 22934575] |
| LNCaP | IC50 |
95 nM
Compound: 28, GDC-0068
|
Cytotoxicity against human LNCAP cells assessed as reduction of resazurin to resorufin after 72 hrs
Cytotoxicity against human LNCAP cells assessed as reduction of resazurin to resorufin after 72 hrs
|
[PMID: 22934575] |
| MCF7 | EC50 |
5036 nM
Compound: Ipatasertib
|
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
|
[PMID: 30996949] |
| MCF7 | IC50 |
1 μM
Compound: 28, GDC-0068
|
Cytotoxicity against human MCF7 cells overexpressing Her2 assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay
Cytotoxicity against human MCF7 cells overexpressing Her2 assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay
|
[PMID: 22934575] |
| MDA-MB-468 | GI50 |
3.7 μM
Compound: GDC-0068
|
Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
|
[PMID: 34855399] |
| NCI-H1975 | IC50 |
>20 μM
Compound: 2; GDC-0068
|
Antiproliferative activity against human osimertinib resistant NCI-H1975 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay
Antiproliferative activity against human osimertinib resistant NCI-H1975 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay
|
[PMID: 36173763] |
| PC-3 | GI50 |
7.6 μM
Compound: GDC-0068
|
Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
|
[PMID: 34855399] |
| PC-3 | IC50 |
1 μM
Compound: 28, GDC-0068
|
Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay
Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay
|
[PMID: 22934575] |
| PC-3 | IC50 |
3544.33 nM
Compound: GDC-0068
|
Antiproliferative activity against human PC-3 habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
Antiproliferative activity against human PC-3 habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
|
[PMID: 35679512] |
| RL95-2 | IC50 |
331.07 nM
Compound: GDC-0068
|
Antiproliferative activity against human RL95-2 habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
Antiproliferative activity against human RL95-2 habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
|
[PMID: 35679512] |
| SMMC-7721 | IC50 |
0.661 μM
Compound: GDC-0068
|
Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability by MTT assay
|
[PMID: 32007668] |
| T47D | EC50 |
443 nM
Compound: Ipatasertib
|
Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
|
[PMID: 30996949] |
| T47D | IC50 |
327.77 nM
Compound: GDC-0068
|
Antiproliferative activity against human T47D habouring PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
Antiproliferative activity against human T47D habouring PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
|
[PMID: 35679512] |
| TOV21G | IC50 |
715.2 nM
Compound: GDC-0068
|
Antiproliferative activity against human TOV-21G habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
Antiproliferative activity against human TOV-21G habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
|
[PMID: 35679512] |
| ZR-75-1 | EC50 |
219 nM
Compound: Ipatasertib
|
Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
|
[PMID: 30996949] |
| ZR-75-1 | IC50 |
1316 nM
Compound: GDC-0068
|
Antiproliferative activity against human ZR-75-1 habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
Antiproliferative activity against human ZR-75-1 habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay
|
[PMID: 35679512] |
Ipatasertib (10 µM; 12, 24 h) suppresses colon cancer cell proliferation by p53 irrespectively activating PUMA in vitro[1].
Ipatasertib (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 increases the mRNA level of PUMA in HCT116 WT, p53−/−, and DLD1 (p53 mutant) cells[1].
Ipatasertib (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 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.
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. 1001264-89-6
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Appearance Solid
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Masse moléculaire 458.00
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Formule C24H32ClN5O2
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Color White to light yellow
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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
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Synonyms
GDC-0068; RG7440
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (63)
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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 -
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 Commun
Attenuated growth factor signaling during cell death initiation sensitizes membranes towards peroxidation. [Abstract]2025 Feb 25;16(1):1774. PMID: 40000627
Ipatasertib 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 -
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 -
Nat Chem Biol
2025 Aug;21(8):1194-1204. PMID: 39934397 -
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 -
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 -
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 -
EMBO Mol Med
2025 Feb;17(2):336-364. PMID: 39748059 -
Haematologica
2020 Mar;105(3):661-673. PMID: 31289202 -
Oncogene
Identification of RAPGEF3 as the therapeutic vulnerability of basal-subtype lung squamous cell carcinoma. [Abstract]2025 Sep;44(34):3142-3148. PMID: 40781157 -
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 -
Br J Cancer
Inhibition of YB-1 phosphorylation enhances cisplatin activity and disrupts cell division in pleural mesothelioma. [Abstract]2025 Sep 4. PMID: 40908296 -
Elife
2020 Dec 7;9:e61405. PMID: 33284104 -
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 -
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 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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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 -
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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 -
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 -
Life Sci
2020 Sep 1;256:117955. PMID: 32534038 -
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 -
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 -
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 -
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 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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Sci Rep
Dendrobium officinale Kimura & Migo polysaccharide ameliorates skin photoaging by promoting angiogenesis. [Abstract]2025 Aug 17;15(1):30048. PMID: 40820014 -
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 -
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 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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Ren Fail
A multi-omics landscape of programmed cell death in acetaminophen-induced acute kidney injury. [Abstract]2025 Dec;47(1):2580064. PMID: 41249093 -
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 -
J Cell Biochem
2024 Aug;125(8):e30613. PMID: 38860522 -
Oncotargets Ther
Inhibition of PI3K-AKT Signaling Blocks PGE2-Induced COX-2 Expression in Lung Adenocarcinoma. [Abstract]2020 Aug 18;13:8197-8208. PMID: 32904445 -
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 Sep 25:223:109692. PMID: 41015102 -
Biochem Biophys Res Commun
Loss of DNA replication fork protection by TIMELESS degradation supports oncogene-induced senescence. [Abstract]2025 Jun 12:776:152203. PMID: 40517672 -
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 -
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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
Solvant et solubilité
DMSO : 100 mg/mL (218.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 3.57 mg/mL (7.79 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (10.92 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (10.92 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. 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. [Content Brief]
[2]. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.1834 mL | 10.9170 mL | 21.8341 mL | 54.5852 mL |
| 5 mM | 0.4367 mL | 2.1834 mL | 4.3668 mL | 10.9170 mL | |
| DMSO | 10 mM | 0.2183 mL | 1.0917 mL | 2.1834 mL | 5.4585 mL |
| 15 mM | 0.1456 mL | 0.7278 mL | 1.4556 mL | 3.6390 mL | |
| 20 mM | 0.1092 mL | 0.5459 mL | 1.0917 mL | 2.7293 mL | |
| 25 mM | 0.0873 mL | 0.4367 mL | 0.8734 mL | 2.1834 mL | |
| 30 mM | 0.0728 mL | 0.3639 mL | 0.7278 mL | 1.8195 mL | |
| 40 mM | 0.0546 mL | 0.2729 mL | 0.5459 mL | 1.3646 mL | |
| 50 mM | 0.0437 mL | 0.2183 mL | 0.4367 mL | 1.0917 mL | |
| 60 mM | 0.0364 mL | 0.1820 mL | 0.3639 mL | 0.9098 mL | |
| 80 mM | 0.0273 mL | 0.1365 mL | 0.2729 mL | 0.6823 mL | |
| 100 mM | 0.0218 mL | 0.1092 mL | 0.2183 mL | 0.5459 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.