2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. Fruquintinib

Fruquintinib  (Synonyms: HMPL-013)

製品番号: HY-19912 純度: 99.98%
COA 取扱説明書 Technical Support

Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 33, 0.35, and 35 nM, respectively.

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CAS 番号 : 1194506-26-7

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>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 67 在庫あり
Solution
10 mM * 1 mL in DMSO USD 67 在庫あり
Solid
5 mg $61 在庫あり
10 mg $99 在庫あり
50 mg $198 在庫あり
100 mg $352 在庫あり
200 mg   お問い合わせ  
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カスタマーレビュー

Based on 10 publication(s) in Google Scholar

Other Forms of Fruquintinib:

Fruquintinib 関連抗体

Top Publications Citing Use of Products

    Fruquintinib purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Dec;31(12):1625-1635.  [Abstract]

    The angiogenesis inhibitor Fruquintinib (Fq) (2 mg/kg; i.g.; once daily) effectively inhibited the expression of CD31 and enhanced the inhibition of 2,5-AM on CD31 in HPAC and MIA Paca2 cell xenograft tumor tissues.

    Fruquintinib purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Dec;31(12):1625-1635.  [Abstract]

    The angiogenesis inhibitor Fruquintinib (Fq) (2 mg/kg; i.g.; once daily) treatment effectively attenuated fructose-induced development of MIA Paca2 cell xenograft tumor.

    Fruquintinib purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2023 Nov 5:259:115703.  [Abstract]

    Representative photographs of tumors and quantification in each group from the HCT116 xenograft model after Fruquintinib (10 mg/kg; p.o) or vehicle treatment.

    Fruquintinib purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2023 Nov 5:259:115703.  [Abstract]

    Representative images and quantification of Ki67, CD68, FAK and E-cad. Fruquintinib (10 mg/kg; p.o) suppressed the proliferation (Ki67 stain) and migration (CD68, FAK, E-cad stain) of tumor cells from the HCT116 xenograft model.

    Fruquintinib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2023 Jun 18:661:10-20.  [Abstract]

    Fruquintinib (2.5 mg/kg; i.g.; once daily for 2 weeks) treatment resulted in slower growth and reduced volume of B16.F1-OVA tumors in C57BL/6 mice.

    VEGFR 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
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    • 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

    Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 33, 0.35, and 35 nM, respectively.

    IC50 & Target[1]

    VEGFR1

    33 nM (IC50)

    VEGFR2

    35 nM (IC50)

    VEGFR3

    0.5 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    COLO 205 IC50
    > 10 3
    Compound: Fruquintinib
    Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay
    Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay
    		[PMID: 35763868]
    COLO 205 IC50
    >10 3
    Compound: Fruquintinib
    Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay
    Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay
    		[PMID: 35763868]
    HCT-116 IC50
    0.8 3
    Compound: Fruquintinib
    Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay
    Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay
    		[PMID: 35763868]
    HT-29 IC50
    1.5 3
    Compound: Fruquintinib
    Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay
    Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay
    		[PMID: 35763868]
    HCT-116 IC50
    0.8 3
    Compound: Fruquintinib
    Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay
    Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay
    		[PMID: 35763868]
    LoVo IC50
    >10 3
    Compound: Fruquintinib
    Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay
    Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay
    		[PMID: 35763868]
    HT-29 IC50
    1.5 3
    Compound: Fruquintinib
    Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay
    Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay
    		[PMID: 35763868]
    LoVo IC50
    > 10 3
    Compound: Fruquintinib
    Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay
    Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay
    		[PMID: 35763868]
    体外実験

    Fruquintinib demonstrates potent inhibition on VEGF-A dependent KDR phosphorylation in HEK293-KDR cells and VEGF-A induced proliferation in primary HUVECs with IC50s of 0.6±0.2 nM and 1.7 nM, respectively. Similarly, potent VEGFR3 attenuation by fruquintinib is observed in primary HLECs, with IC50s of 1.5 nM and 4.2 nM for VEGF-C stimulated VEGFR3 phosphorylation and proliferation, respectively. Fruquintinib suppresses the tube branching, tube length and area in a concentration-dependent manner. The tubule length of primary HUVECs decreased by 74% and 94% at 0.03 and 0.3 μM of fruquintinib, respectively. Fruquintinib inhibits HUVEC tubule growth and CAM angiogenesis. Tube formation is suppressed significantly after treatment with fruquintinib at 0.3 μM for 18 hours[1].

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

    Fruquintinib 関連抗体
    体内実験

    Gastric cancer BGC-823 model is found to be most sensitive to fruquintinib. In this model, fruquintinib inhibits tumor growth by 62.3% and 95.4～98.6%, at 0.5 and 2 mg/kg once daily dosing, respectively. When the dose is elevated to 5 mg/kg and 20 mg/kg, the tumors regress by 24.1% and 48.6%, respectively. The level of anti-tumor growth activity of fruquintinib varies in different tumor xenograft models. Fruquintinib significantly decreases the micro-vessel density even at the lowest dose of 0.8 mg/kg[1].

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

    393.39

    分子式

    C21H19N3O5
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=C(C)OC2=CC(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)=CC=C12)NC
    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 : 5 mg/mL (12.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5420 mL 12.7100 mL 25.4201 mL
    5 mM 0.5084 mL 2.5420 mL 5.0840 mL
    10 mM 0.2542 mL 1.2710 mL 2.5420 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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: ≥ 0.33 mg/mL (0.84 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.33 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 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: ≥ 0.33 mg/mL (0.84 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.33 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 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: 99.98%

    COA (260 KB) HNMR (261 KB) RP-HPLC (221 KB) LCMS (100 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [1]

    Primary HUVECs or HLECs in exponential phase are suspended in 100 μL of RPMI-1640 media containing 0.5% FBS, and seeded at 5000 cell/well in 96-well plates pre-coated with 0.2% gelatin or fibronectin, and incubated overnight in a 5% CO2, 37°C incubator. Fruquintinib and VEGF-A165 or VEGF-C (50 ng/mL) are added and incubated for 48 hours. Viability of the cells is determined using CCK-8 assay format[1].

    MedChemExpress (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
    [1]

    Mice: The patient derived xenograft models are established after the primary tumor adopted serial passages in vivo. Once tumors have grown to 100-300 mm3, the animals are randomly assigned with 6-8 animals per group. The mice are treated orally with the vehicle (control group) or fruquintinib at a dose range of 0.5-20 mg/kg suspended in the vehicle (treated group) once daily for 3 weeks. In combination studies, docetaxel (Taxotere, 5 mg/kg) or oxaliplatin (10 mg/kg) is administered to nude mouse via intravenous injection, once a week. Tumor size and body weights are measured 3 times a week. Tumor volumes (TV) are calculated[1].

    MedChemExpress (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

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5420 mL 12.7100 mL 25.4201 mL 63.5502 mL
    5 mM 0.5084 mL 2.5420 mL 5.0840 mL 12.7100 mL
    10 mM 0.2542 mL 1.2710 mL 2.5420 mL 6.3550 mL
    • No file chosen (Maximum size is: 1024 Kb)
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    Fruquintinib 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:

    Fruquintinib1194506-26-7HMPL-013HMPL013HMPL 013VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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