Ipatasertib dihydrochloride (Synonyms: GDC-0068 dihydrochloride; RG-7440 dihydrochloride)

Name: Ipatasertib dihydrochloride
Brand: MedChemExpress
SKU: HY-15186A
Rating: 5.0 (42 reviews)

Cat. No.: HY-15186A Purity: 99.09%: FAQs
Data Sheet SDS COA Handling Instructions

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Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC₅₀s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.

For research use only. We do not sell to patients.

Ipatasertib dihydrochloride Chemical Structure

CAS No. : 1396257-94-5

Size	Price	Stock	Quantity

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 82	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 82	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
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Based on 42 publication(s) in Google Scholar

Other Forms of Ipatasertib dihydrochloride:

39 Publications Citing Use of MCE Ipatasertib dihydrochloride

: Ipatasertib dihydrochloride 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 dihydrochloride 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.

: Ipatasertib dihydrochloride 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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View All Isoforms

Akt Akt1 Akt2 Akt3

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Akt1

5 nM (IC₅₀)

Akt3

8 nM (IC₅₀)

Akt2

18 nM (IC₅₀)

PKA

3100 nM (IC₅₀)

In Vitro

Ipatasertib shows more than 600 and more than 100-fold selectivity for Akt1 in IC₅₀ against the closely related kinases PKA and p70S6K, respectively. When tested at 1 μM in a panel of 230 protein kinases, which includes 36 human AGC family members, Ipatasertib inhibits only 3 other kinases by more than 70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K). IC₅₀s measured for these 3 kinases are 98, 69, and 860 nM, respectively. Thus, with the exception of PKG1 (relative to which Ipatasertib is >10-fold more selective for Akt1), Ipatasertib displays a more than 100-fold selectivity for Akt1 over the next most potently inhibited non-Akt kinase, p70S6K, in the screening kinase panel. The relationship between pharmacokinetics (PK) and pharmacodynamics (PD) of Ipatasertib is investigated in 3 xenograft models that showed dose-dependent response to drug treatment: MCF7-neo/HER2, TOV-21G.x1, and LNCaP. The mean cell viability IC₅₀ of Ipatasertib in these 3 cell lines is 2.56, 0.44, and 0.11 μM, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ipatasertib is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression is achieved at or below 100 mg/kg daily oral dose, which is the maximum dose tested in immunocompromised mice that is well tolerated. When tested in vivo, daily dosing of Ipatasertib in combination with RP-56976 induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where each single agent is ineffective or only causes modest tumor growth delay. Similarly, increased TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib is combined with NSC 241240. The combination of Ipatasertib with RP-56976 or NSC 241240 is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

530.92

Formula

C₂₄H₃₄Cl₃N₅O₂

CAS No.

1396257-94-5

Appearance

Solid

Color

Light yellow to yellow

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.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (188.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 41 mg/mL (77.22 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8835 mL	9.4176 mL	18.8352 mL
5 mM	0.3767 mL	1.8835 mL	3.7670 mL
10 mM	0.1884 mL	0.9418 mL	1.8835 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 3.88 mg/mL (7.31 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.88 mg/mL (7.31 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO 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 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

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 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn 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: PBS
Solubility: 16.67 mg/mL (31.40 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.27%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (254 KB) HNMR (271 KB) RP-HPLC (144 KB) LCMS (128 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[2]. Lin J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72. [Content Brief]

Cell Assay ^[2]	The 384-well plates are seeded with 2,000 cells per well in a volume of 54 μL per well followed by incubation at 37°C under 5% CO₂ overnight (~16 hours). Compounds (e.g., Ipatasertib) are diluted in DMSO to generate the desired stock concentrations then added in a volume of 6 μL per well. All treatments are tested in quadruplicates. After 4 days incubation, relative numbers of viable cells are estimated using CellTiter-Glo and total luminescence is measured on a Wallac Multilabel Reader. The concentration of drug resulting in IC₅₀ is calculated from a 4-parameter curve analysis (XLfit) and is determined from a minimum of 3 experiments. For cell lines that failed to achieve an IC₅₀, the highest concentration tested (10 μM) is listed^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] In vivo efficacy is evaluated in multiple tumor cell line- and patient-derived xenograft models. Cells or tumor fragments are implanted subcutaneously into the flank of immunocompromised mice. Female or male nude (nu/nu) or severe combined immunodeficient mice (SCID)/beige mice are used. The LuCaP35V patient-derived primary tumors are obtained; male mice are castrated before implantation of tumor fragments. After implantation of tumor cells or fragments into mice, tumors are monitored until they reached mean tumor volumes of 180 to 350 mm³ and distributed into groups of 8 to 10 animals/group. Ipatasertib is formulated in 0.5% methylcellulose/0.2% Tween-80 (MCT) and administered daily (QD), via oral (per os; PO) gavage. RP-56976 is formulated in 3% EtOH/97% saline and dosed intravenously (IV) every week (QW) at 2.5 or 7.5 mg/kg. NSC 241240 is formulated in saline and dosed intraperitoneally (IP) weekly at 50 mg/kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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. [Content Brief] [2]. Lin J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.8835 mL	9.4176 mL	18.8352 mL	47.0881 mL
	5 mM	0.3767 mL	1.8835 mL	3.7670 mL	9.4176 mL
	10 mM	0.1884 mL	0.9418 mL	1.8835 mL	4.7088 mL
	15 mM	0.1256 mL	0.6278 mL	1.2557 mL	3.1392 mL
	20 mM	0.0942 mL	0.4709 mL	0.9418 mL	2.3544 mL
	25 mM	0.0753 mL	0.3767 mL	0.7534 mL	1.8835 mL
	30 mM	0.0628 mL	0.3139 mL	0.6278 mL	1.5696 mL
	40 mM	0.0471 mL	0.2354 mL	0.4709 mL	1.1772 mL
	50 mM	0.0377 mL	0.1884 mL	0.3767 mL	0.9418 mL
	60 mM	0.0314 mL	0.1570 mL	0.3139 mL	0.7848 mL
DMSO	80 mM	0.0235 mL	0.1177 mL	0.2354 mL	0.5886 mL
DMSO	100 mM	0.0188 mL	0.0942 mL	0.1884 mL	0.4709 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 dihydrochloride 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.

Keywords:

Ipatasertib1396257-94-5GDC-0068RG-7440GDC0068GDC 0068RG7440RG 7440OrganoidAktPKBProtein kinase BInhibitorinhibitorinhibit

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Ipatasertib dihydrochloride (Synonyms: GDC-0068 dihydrochloride; RG-7440 dihydrochloride)

Customer Review

Other Forms of Ipatasertib dihydrochloride:

Ipatasertib dihydrochloride Related Antibodies

39 Publications Citing Use of MCE Ipatasertib dihydrochloride

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Akt Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Ipatasertib dihydrochloride Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Ipatasertib dihydrochloride Related Classifications

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