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

Bemcentinib  (Synonyms: R428; BGB324)

Cat. No.: HY-15150 Purity: 99.92%
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Bemcentinib (R428) est un inhibiteur puissant et sélectif de Axl avec un IC50 de 14 nM.

Bemcentinib (R428) ist ein starker und selektiver Inhibitor von Axl mit einem IC50 von 14 nM.

Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM.

For research use only. We do not sell to patients.

Bemcentinib Chemical Structure

Bemcentinib Chemical Structure

CAS No. : 1037624-75-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 111 In-stock
Solution
10 mM * 1 mL in DMSO USD 111 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 100 In-stock
10 mg USD 180 In-stock
50 mg USD 350 In-stock
100 mg USD 600 In-stock
200 mg   Get quote  
500 mg   Get quote  

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

Customer Review

Based on 47 publication(s) in Google Scholar

Other Forms of Bemcentinib:

Bemcentinib Related Antibodies

Top Publications Citing Use of Products

41 Publications Citing Use of MCE Bemcentinib

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 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: 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: 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.

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    Axl Mer Tyro3

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM[2].

    IC50 & Target

    Axl

     

    In Vitro

    Bemcentinib (R428) (2μM) 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 Related Antibodies
    In Vivo

    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.
    Clinical Trial
    Molecular Weight

    506.64

    Formula

    C30H34N8
    CAS No.
    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    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
    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
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.11 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  0.5% CMC-Na/saline water

      Solubility: 12.5 mg/mL (24.67 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% HPMC/1% Tween-80 in Saline water

      Solubility: 5 mg/mL (9.87 mM); Suspended solution; Need ultrasonic

    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.
    Purity & Documentation

    Purity: 99.92%

    COA (260 KB) HNMR (300 KB) RP-HPLC (243 KB) LCMS (100 KB) Elemental Analysis Report (117 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [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.

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

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

    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

    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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