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

Bemcentinib (Synonyms: R428; BGB324)

Cat. No.: HY-15150 Purity: 99.76% ee.: 99.63%
Handling Instructions

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

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10 mM * 1 mL in DMSO USD 111 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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 MCE. Usage Cited in: Oncotarget. 2017 Jun 20;8(25):41064-41077.

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

    Bemcentinib purchased from MCE. Usage Cited in: Sci Rep. 2017 Dec 19;7(1):17770.

    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 MCE. Usage Cited in: Cancer Cell. 2018 Dec 10;34(6):954-969.e4.

    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 MCE. Usage Cited in: Cancer Cell. 2018 Dec 10;34(6):954-969.e4.

    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.
    • Biological Activity

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    Description

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

    IC50 & Target

    IC50: 14 nM (Axl kinase)

    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-1μM) causes a concentration-dependent inhibition of preadipocyte differentiation into mature adipocytes, as evidenced by reduced lipid uptake[3].

    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].

    Clinical Trial
    Molecular Weight

    506.64

    Formula

    C₃₀H₃₄N₈

    CAS No.

    1037624-75-1

    SMILES

    NC1=NC(NC2=CC(CC[[email protected]@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 : 10.25 mg/mL (20.23 mM; Need ultrasonic and warming)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.71 mg/mL (1.40 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 0.71 mg/mL (1.40 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 0.71 mg/mL (1.40 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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.

    Purity: 99.76% ee.: 99.63%

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    Keywords:

    BemcentinibR428BGB324R 428R-428BGB 324BGB-324TAM ReceptorTyro3AxlMerInhibitorinhibitorinhibit

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    Product name:
    Bemcentinib
    Cat. No.:
    HY-15150
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