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  3. Ipatasertib

Ipatasertib (Synonyms: GDC-0068; RG7440)

Cat. No.: HY-15186 Purity: 98.42%
Handling Instructions

Ipatasertib (GDC-0068) 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 Chemical Structure

Ipatasertib Chemical Structure

CAS No. : 1001264-89-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 71 In-stock
Estimated Time of Arrival: December 31
2 mg USD 50 In-stock
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5 mg USD 70 In-stock
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10 mg USD 100 In-stock
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50 mg USD 290 In-stock
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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
1 g USD 2600 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

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Description

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

IC50 & Target[1]

Akt1

5 nM (IC50)

Akt3

8 nM (IC50)

Akt2

18 nM (IC50)

PKA

3100 nM (IC50)

In Vitro

Ipatasertib (GDC-0068) 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, GDC-0068 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 (GDC-0068) is >10-fold more selective for Akt1), Ipatasertib (GDC-0068) 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 (GDC-0068) 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 GDC-0068 in these 3 cell lines is 2.56, 0.44, and 0.11 μM, respectively[2].

In Vivo

Ipatasertib (GDC-0068) 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 (GDC-0068) in combination with Docetaxel 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 (GDC-0068) is combined with Carboplatin. The combination of Ipatasertib (GDC-0068) with Docetaxel or Carboplatin is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone[2].

Clinical Trial
Molecular Weight

458.00

Formula

C₂₄H₃₂ClN₅O₂

CAS No.

1001264-89-6

SMILES

ClC1=CC=C([[email protected]@H](CNC(C)C)C(N2CCN(C3=C([[email protected]](C)C[[email protected]]4O)C4=NC=N3)CC2)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 28 mg/mL (61.14 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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 (GDC-0068)) 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. For the MCF7-neo/HER2 model, 17β-estradiol pellets (0.36 mg/pellet, 60-day release) are implanted into the dorsal shoulder before cell inoculation. 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 (GDC-0068) is formulated in 0.5% methylcellulose/0.2% Tween-80 (MCT) and administered daily (QD), via oral (per os; PO) gavage. Docetaxel is formulated in 3% EtOH/97% saline and dosed intravenously (IV) every week (QW) at 2.5 or 7.5 mg/kg. Carboplatin 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

Purity: 98.42%

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Ipatasertib
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HY-15186
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