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.
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Ipatasertib Chemical Structure
CAS No. : 1001264-89-6
This product is a controlled substance and not for sale in your territory.
Based on 38 publication(s) in Google Scholar
Other Forms of Ipatasertib:
Ipatasertib dihydrochloride
In-stock
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.
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.
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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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].
IC50 & Target[2]
Akt1
5 nM (IC50)
Akt3
8 nM (IC50)
Akt2
18 nM (IC50)
PKA
3100 nM (IC50)
In Vitro
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.
Ipatasertib Related Antibodies
Cell Viability Assay[1]
Cell Line:
HCT116 WT, p53−/−, and DLD1 (p53 mutant) cells
Concentration:
10 µM
Incubation Time:
12, 24 h
Result:
Decreased all the three cell lines viability.
Apoptosis Analysis[1]
Cell Line:
HCT116 cells
Concentration:
10 µM
Incubation Time:
24 h
Result:
Induced apoptosis through PUMA/Bax pathway.
Western Blot Analysis[1]
Cell Line:
HCT116 cells
Concentration:
1, 5, 10, 20 μM for 24 h/10 μM for 3, 6, 12, 24 h
Incubation Time:
24 h; 3, 6, 12, 24 h
Result:
Increased the level of PUMA in a concentration and time dependent manner.
In Vivo
Ipatasertib (30 mg/kg; p.o.; single daily for 15 consecutive days) exhibits PUMA-dependent antitumor activity in HCT116 WT and PUMA−/− cells xenograft nude mice model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
HCT116 WT and PUMA−/− cells xenograft nude mice model[1].
Dosage:
30 mg/kg
Administration:
Oral gavage; single daily for 15 consecutive days.
Result:
Inhibited growth of tumors in a PUMA-dependent manner.
Room temperature in continental US; may vary elsewhere.
Stockage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
2 years
-20°C
1 year
Solvant et solubilité
In Vitro:
DMSO : 220 mg/mL (480.35 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)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.1834 mL
10.9170 mL
21.8341 mL
5 mM
0.4367 mL
2.1834 mL
4.3668 mL
10 mM
0.2183 mL
1.0917 mL
2.1834 mL
View the 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.
*
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.
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.
Protocol 1
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 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.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. 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.
Protocol 1
Add each solvent one by one: 0.5% Methyl cellulose/0.5% Tween-80 in Saline water
Solubility: 10 mg/mL (21.83 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
[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]
[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.
[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.
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
ConcentrationSolventMass
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.
Ipatasertib Related Classifications
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.