2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. Bemcentinib

Bemcentinib  (Synonyms: R428; BGB324)

製品番号: HY-15150 純度: 99.92%
COA 取扱説明書 Technical Support

Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer.

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CAS 番号 : 1037624-75-1

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 111 在庫あり
Solution
10 mM * 1 mL in DMSO USD 111 在庫あり
Solid
5 mg $100 在庫あり
10 mg $180 在庫あり
50 mg $350 在庫あり
100 mg $600 在庫あり
200 mg $930 在庫あり
500 mg   お問い合わせ  
1 g   お問い合わせ  

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カスタマーレビュー

Based on 62 publication(s) in Google Scholar

Other Forms of Bemcentinib:

Bemcentinib 関連抗体

Top Publications Citing Use of Products

顧客検証

WB

    Bemcentinib purchased from MedChemExpress. Usage Cited in: Mil Med Res. 2023 Feb 22;10(1):7.  [Abstract]

    Bemcentinib (BGB324; 1 μM; 30 min) partially blocks the activation of HSC by rGAS6 in LX-2 cells.

    Bemcentinib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2018 Dec 10;34(6):954-969.e4.  [Abstract]

    Western blot showing phosphorylated PLCγ2 in cells treated with gef (1 μM) and R428 or Lapa for 24 hr. SE, short exposure; LE, long exposure.

    Bemcentinib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2018 Dec 10;34(6):954-969.e4.  [Abstract]

    Western blot showing PKCδ expression in nuclear extracts of GR4 and GR10 cells treated with 1 μM gef in combination with 2.5 μM R428 and 5 μM GW572016 (Lapa) for 24 hr.

    Bemcentinib purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of TAM receptor (LDC1267 at 1 µM, UNC2250 at 5 µM, R428 at 5 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

    Bemcentinib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Dec 19;7(1):17770.  [Abstract]

    Western blot analysis of pAXL level in H1299 cells treated with the indicated concentration of R428 for 1 h. Results are confirmed in three independent experiments.

    Bemcentinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jun 20;8(25):41064-41077.  [Abstract]

    The expression of AXL in the PC3-DR and DU145-DR cells treated with R428 (1 μM) is analyzed by western blotting.

    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

    • 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

    Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer[1][2].

    IC50 & Target

    Axl

     

    Cellular Effect
    Cell Line Type Value Description References
    4T1 IC50
    0.94 μM
    Compound: 1; R428, BGB-324
    Antiproliferative activity against mouse 4T1 cells highly expressing AXL after 72 hrs by MTT assay
    Antiproliferative activity against mouse 4T1 cells highly expressing AXL after 72 hrs by MTT assay
    		[PMID: 35279611]
    BaF3 IC50
    117.2 nM
    Compound: 8; R428; BGB324
    Antiproliferative activity against mouse BaF3 stably expressing human TEL-AXL incubated for 72 hrs
    Antiproliferative activity against mouse BaF3 stably expressing human TEL-AXL incubated for 72 hrs
    		[PMID: 33957388]
    BaF3 IC50
    117.2 nM
    Compound: 2; BGB324
    Antiproliferative activity against mouse BaF3/TEL-AXL cells incubated for 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BaF3/TEL-AXL cells incubated for 72 hrs by SRB or CCK8 assay
    		[PMID: 33733758]
    BaF3 IC50
    98.8 nM
    Compound: 1; BGB324
    Antiproliferative activity against mouse BaF3 cells transfected with TEL-AXL assessed as inhibition of cell growth incubated for 72 hrs
    Antiproliferative activity against mouse BaF3 cells transfected with TEL-AXL assessed as inhibition of cell growth incubated for 72 hrs
    		[PMID: 36358010]
    GES1 IC50
    >60 μM
    Compound: 1; R428, BGB-324
    Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
    Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
    		[PMID: 35279611]
    HeLa IC50
    <30 nM
    Compound: 17; BGB324; R428
    Inhibition of recombinant AXL in human HeLa cells after 1 hr by ELISA
    Inhibition of recombinant AXL in human HeLa cells after 1 hr by ELISA
    		[PMID: 26555154]
    MCF-10A IC50
    >60 μM
    Compound: 1; R428, BGB-324
    Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
    Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
    		[PMID: 35279611]
    MDA-MB-231 IC50
    2.84 μM
    Compound: 1; R428, BGB-324
    Antiproliferative activity against human MDA-MB-231 cells highly expressing AXL after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells highly expressing AXL after 72 hrs by MTT assay
    		[PMID: 35279611]
    体外実験

    Bemcentinib (R428) (2 μM) significantly interferes with mechanisms of migration and invasion of Axlpos melanoma cells at levels comparable to Axl knockdown[1].
    Bemcentinib (R428) synergizes with CDDP to enhance suppression of liver micrometastasis[2].
    Bemcentinib (R428) (50 nM-1 μM) causes a concentration-dependent inhibition of preadipocyte differentiation into mature adipocytes, as evidenced by reduced lipid uptake[3].

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

    Bemcentinib 関連抗体
    体内実験

    Bemcentinib (R428) (125 mg/kg, p.o.) significantly blocks MDA-MB-231-luc-D3H2LN metastases development in two independent mouse models of breast cancer dissemination, suppresses both tumor angiogenesis and vascular endothelial growth factor (VEGF)-induced corneal neovascularization in vivo[2].
    Bemcentinib (R428) (75 mg/kg/day, 25 mg/kg twice daily, p.o.) makes mice keep on a high-fat diet resulted in significantly reduced weight gain and subcutaneous and gonadal fat mass[3].

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

    506.64

    分子式

    C30H34N8
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    NC1=NC(NC2=CC(CC[C@@H](N3CCCC3)CC4)=C4C=C2)=NN1C(N=N5)=CC6=C5C7=CC=CC=C7CCC6
    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 : 12.5 mg/mL (24.67 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 1.9738 mL 9.8689 mL 19.7379 mL
    5 mM 0.3948 mL 1.9738 mL 3.9476 mL
    10 mM 0.1974 mL 0.9869 mL 1.9738 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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: ≥ 1.25 mg/mL (2.47 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
    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: 99.92%

    COA (260 KB) HNMR (300 KB) RP-HPLC (242 KB) LCMS (99 KB) Elemental Analysis Report (117 KB)

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

    Cells maintained for 24 hours in serum-free medium are harvested and transferred to the upper chamber (1.5×105 cells per well) of uncoated (migration) or matrigel-coated (invasion) 24-well chambers. RPMI medium containing 10% fetal bovine serum is added to the lower chamber. Bemcentinib (R428) (2 μM) or vehicle (DMSO, 0.25%) is added for 2 hours to cells before loading them in the upper chambers. Both the upper and lower chambers contain the drug or vehicle. Quantification of migrating/invading cells is obtained by measuring their fluorescent signals with a 480/520 nm filter set on an Infinite M1000 microplate reader 20 or 42 hours later, respectively.

    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
    [2]

    Seven- to 8-wk-old female NCr nu/nu mice are injected intracardially with bioluminescent MDA-MB-231-luc-D3H2LN cell suspension. Oral dosing with Bemcentinib (R428) (125 mg/kg, p.o.) or vehicle twice daily begins 2 h before cell implantation and continue to day 21 (n=20). Metastatic burden is quantified by in vivo bioluminescence imaging on day 22 and analyzed using the Wilcoxon rank sum test.

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

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9738 mL 9.8689 mL 19.7379 mL 49.3447 mL
    5 mM 0.3948 mL 1.9738 mL 3.9476 mL 9.8689 mL
    10 mM 0.1974 mL 0.9869 mL 1.9738 mL 4.9345 mL
    15 mM 0.1316 mL 0.6579 mL 1.3159 mL 3.2896 mL
    20 mM 0.0987 mL 0.4934 mL 0.9869 mL 2.4672 mL
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    Bemcentinib 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:

    Bemcentinib1037624-75-1R428 BGB324R 428R-428BGB324BGB 324BGB-324TAM ReceptorTyro3AxlMerInhibitorinhibitorinhibit

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    製品番号:
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