1. PI3K/Akt/mTOR
  2. Akt
  3. Ipatasertib

Ipatasertib (Synonyms: GDC-0068; RG7440)

製品番号: HY-15186 純度: 98.42%
取扱説明書

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.

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Ipatasertib 構造式

Ipatasertib 構造式

CAS 番号 : 1001264-89-6

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 71 在庫あり
Estimated Time of Arrival: December 31
2 mg USD 50 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 70 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 100 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 290 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 450 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 750 在庫あり
Estimated Time of Arrival: December 31
500 mg USD 1500 在庫あり
Estimated Time of Arrival: December 31
1 g USD 2600 在庫あり
Estimated Time of Arrival: December 31
5 g   お問い合わせ  
10 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 18 publication(s) in Google Scholar

Other Forms of Ipatasertib:

Top Publications Citing Use of Products

    Ipatasertib purchased from MCE. Usage Cited in: Biochem Pharmacol. 2020 Jul 9;114145.

    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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    • 参考文献

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    製品説明

    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)

    体外実験

    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].

    体内実験

    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 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 (GDC-0068) is combined with NSC 241240. The combination of Ipatasertib (GDC-0068) 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].

    臨床実験
    分子量

    458.00

    分子式

    C₂₄H₃₂ClN₅O₂

    CAS 番号

    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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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.
    体内:
    • 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.
    参考文献
    細胞実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [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 (GDC-0068) 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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 98.42%

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    Keywords:

    IpatasertibGDC-0068RG7440GDC0068GDC 0068RG 7440RG-7440AktPKBProtein kinase BInhibitorinhibitorinhibit

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    製品名:
    Ipatasertib
    製品番号:
    HY-15186
    数量:
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