2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. SGI-7079

SGI-7079 is a selective, ATP-competitive, orally active inhibitor of the receptor tyrosine kinase Axl. SGI-7079 blocks Axl-mediated signaling pathways such as NF-κB activation and MMP-9 expression, thereby inhibiting tumor cell proliferation, migration and invasion. SGI-7079 is mainly used in the research of malignant tumors such as inflammatory breast cancer and bladder cancer, as well as in combination with immunization (used in combination with PD-1 therapy)[1][2][3].

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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。

CAS 番号 : 1239875-86-5

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 77 在庫あり
Solution
10 mM * 1 mL in DMSO USD 77 在庫あり
Solid
5 mg $70 在庫あり
10 mg $120 在庫あり
25 mg $250 在庫あり
50 mg $310 在庫あり
100 mg $450 在庫あり
200 mg   お問い合わせ  
500 mg   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 3 publication(s) in Google Scholar

SGI-7079 関連抗体

Top Publications Citing Use of Products

    SGI-7079 purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2023 Jan 18;188:106668.  [Abstract]

    SGI-7079 (1 μM; 24 h) effectively inhibits AXL activation in HCC827/OR and H1975/OR cells.

    TAM Receptor 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
    Axl Mer Tyro3

    • 生物活性

    • 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

    SGI-7079 is a selective, ATP-competitive, orally active inhibitor of the receptor tyrosine kinase Axl. SGI-7079 blocks Axl-mediated signaling pathways such as NF-κB activation and MMP-9 expression, thereby inhibiting tumor cell proliferation, migration and invasion. SGI-7079 is mainly used in the research of malignant tumors such as inflammatory breast cancer and bladder cancer, as well as in combination with immunization (used in combination with PD-1 therapy)[1][2][3].

    IC50 & Target

    Axl

     

    体外実験

    SGI-7079 significantly inhibits the proliferation of SUM149 and KPL-4 breast cancer cells with IC50 of 0.43 μM and 0.16 μM at 72 h, respectively[1].
    SGI-7079 (0.25 μM, 0.5 μM; 18 h) significantly reduces the migration and invasion abilities of SUM149 cells[1].
    SGI-7079 (1 μM; 5 h) blocks Gas6-induced Axl (Tyr702) phosphorylation[1].
    SGI-7079 (0.25 μM, 0.5 μM; 48 h) inhibits cell cycle arrest at G1/S phase in KPL-4 cells[1].

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

    SGI-7079 関連抗体
    体内実験

    SGI-7079 (50 mg/kg; oral; 5 days a week for 2 weeks) significantly inhibits tumor growth and prolongs survival in the SUM149 inflammatory breast cancer subcutaneous xenograft model in mice[3].
    SGI-7079 (50 mg/kg; oral; 5 days a week for 2 weeks) combined with anti-PD-1 antibody, induces tumor eradication in the mouse ID8 ovarian cancer peritoneal model, with one-third of the mice surviving long-term[3].

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

    455.53

    分子式

    C26H26FN7
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    N#CCC1=CC=CC(C2=C3C(NC=C3C)=NC(NC4=CC=C(N5CCN(C)CC5)C(F)=C4)=N2)=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 : ≥ 34 mg/mL (74.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1952 mL 10.9762 mL 21.9525 mL
    5 mM 0.4390 mL 2.1952 mL 4.3905 mL
    10 mM 0.2195 mL 1.0976 mL 2.1952 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.17 mg/mL (4.76 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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)

      Solubility: ≥ 2.17 mg/mL (4.76 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
    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.
     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.
    純度とドキュメンテーション

    純度: 99.32%

    COA (252 KB) HNMR (153 KB) LCMS (95 KB)

    取扱説明書 (2659 KB)
    参考文献

    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 Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1952 mL 10.9762 mL 21.9525 mL 54.8811 mL
    5 mM 0.4390 mL 2.1952 mL 4.3905 mL 10.9762 mL
    10 mM 0.2195 mL 1.0976 mL 2.1952 mL 5.4881 mL
    15 mM 0.1463 mL 0.7317 mL 1.4635 mL 3.6587 mL
    20 mM 0.1098 mL 0.5488 mL 1.0976 mL 2.7441 mL
    25 mM 0.0878 mL 0.4390 mL 0.8781 mL 2.1952 mL
    30 mM 0.0732 mL 0.3659 mL 0.7317 mL 1.8294 mL
    40 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3720 mL
    50 mM 0.0439 mL 0.2195 mL 0.4390 mL 1.0976 mL
    60 mM 0.0366 mL 0.1829 mL 0.3659 mL 0.9147 mL
    • 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.

    SGI-7079 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    SGI-70791239875-86-5SGI7079SGI 7079TAM ReceptorTyro3AxlMerInhibitorinhibitorinhibit

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    製品名:
    SGI-7079
    製品番号:
    HY-12964
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