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

Ipatasertib  (Synonyms: GDC-0068; RG7440)

製品番号: HY-15186 純度: 99.88%
COA 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

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
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solution
10 mM * 1 mL in DMSO USD 71 在庫あり
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 71 在庫あり
Solid
2 mg USD 50 在庫あり
5 mg USD 70 在庫あり
10 mg USD 100 在庫あり
50 mg USD 290 在庫あり
100 mg USD 450 在庫あり
200 mg USD 750 在庫あり
500 mg USD 1500 在庫あり
1 g USD 2600 在庫あり
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

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 29 publication(s) in Google Scholar

Other Forms of Ipatasertib:

Top Publications Citing Use of Products

顧客検証

WB

    Ipatasertib purchased from MCE. 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 purchased from MCE. 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.

    Akt アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Akt Akt1 Akt2 Akt3

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    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].

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

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    458.00

    Appearance

    Solid

    分子式

    C24H32ClN5O2
    CAS 番号
    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 : 220 mg/mL (480.35 mM; Need ultrasonic)

    H2O : 3.57 mg/mL (7.79 mM; ultrasonic and warming and heat to 60°C)

    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:  0.5% MC  0.5% Tween-80

      Solubility: 10 mg/mL (21.83 mM); Suspended solution; Need ultrasonic

    • 2.

      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

    • 3.

      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

    • 4.

      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 available by MCE.
    純度とドキュメンテーション

    純度: 99.88%

    COA (252 KB) HNMR (258 KB) RP-HPLC (294 KB) MS (82 KB)

    取扱説明書 (2659 KB)
    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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    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.

    • モル濃度カルキュレーター

    • 希釈カルキュレーター

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    Ipatasertib1001264-89-6GDC-0068 RG7440GDC0068GDC 0068RG7440RG 7440RG-7440AktPKBProtein kinase BInhibitorinhibitorinhibit

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

    		  

    タイトル

    お名前 *

    		 

    PC 用メールアドレス *

    電話番号 *

    		 

    勤務先/学校名 *

    Department *

    		 

    カスタマ需要量 *

    国会或いは地域 *

    		      

    必ず会社名を記載ください。個人への返信は行いません。

    メッセージ

    バルクお問い合わせ

    Inquiry Information

    製品名:
    Ipatasertib
    製品番号:
    HY-15186
    数量:
    MCE 日本正規代理店:

    カスタマーレビュー

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    製品名

    		  

    Lot #

    お名前 *

    		 

    PC 用メールアドレス *

    電話番号 *

    		 

    部門 *

    勤務先/学校名 *

    		 

    国会或いは地域 *

    メッセージ

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.