R428 (BGB324|Bemcentinib)

Catalog No.S2841

R428 (BGB324|Bemcentinib) Chemical Structure

Molecular Weight(MW): 506.64

R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

Size Price Stock Quantity  
USD 370 In stock
USD 870 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 28 Publications

Purity & Quality Control

Choose Selective TAM Receptor Inhibitors

Biological Activity

Description R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).
Targets
Axl [1]
(Cell-free assay)
14 nM
In vitro

R428 blocks the catalytic and procancerous activities of Axl. R428 inhibits Axl with low nanomolar activity and blocks Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. [1] In a recent study, the Axl inhibitor R428 shows a mean IC50 dose of ∼ 2.0μM for the primary CLL B cells after 24 hours of treatment and normal B-, T-, and natural killer (NK) cells show no significant amount of cell death at this dose of R428 (2.5 μM) under similar experimental conditions. [2]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells MlXTSpVv[3Srb36gZZN{[Xl? NXq2VXViOSCq MW\Jcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IFHYUEBqdiCqdX3hckBJ\UyjIHPlcIx{KGGodHXyJFEhcHJiYomgSWxKW0FuIFnDOVA:OC5yMzFOwG0> NH3Mb2QzPjV3NUG1OC=>
H1299 MYDHdo94fGhiaX7obYJqfG:wIHHzd4F6 Moe0OFghcA>? MkKwVlQzQCCrbnjpZol1\WRiZ4Lve5RpKG:oIFixNlk6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKHerdHigZY4hUUN3MDDv[kBieHC{b4jpcYF1\Wy7IESg{txONg>? MmXUN|AzOTB7MUe=
LM3 cells NXjrU2VVTnWwY4Tpc44h[XO|YYm= MWeyMlUh|ryP MY[wMVM3KGh? MUfSOFI5KGmwZIXj[YQh[3m2b4DsZZNucWNidnHjeY9t\XNid3n0bIlvKG:wZTDoc5VzKGGodHXyJHI1OjhidILlZZRu\W62LDDhcoQhfGinII\hZ5VwdGW|IHnuZ5Jm[XOnZDDpckBvfW2kZYKgZY5lKHOrenWge4l1cCC2aX3lMi=> MUSzNFIyODlzNx?=
Bel7404 cells MXfGeY5kfGmxbjDhd5NigQ>? NGrieFQyKM7:TR?= M4HINFQ5KGh? Mlf1VlQzQCCjbITldoVlKHSqZTDsfZNwe2:vYXygdGgh[W6mIHLsc4Ns\WRiYYX0c5Bp[WerYzDk[Ydz[WSjdHnvck4> M3n2NlMxOjFyOUG3
A549 cells NVXKU21STnWwY4Tpc44h[XO|YYm= Mo\GNlQhcA>? MnHYZ49v[2:vaYThcpQhfHKnYYTt[Y51KG:oIITo[UBk\WyuczD3bZRpKFJ2MkigZY5lKGKjZnnsc416[2mwIDjCZYYhSTFrIH;yJINpdG:{b4H1bY5mKCiFUTmgZYxt\X[rYYTl[EB1cGVidnHjeY9tcXqjdHnvckBqdmS3Y3XkJIJ6KFJ2Mkiu NXnkPYU2OzB{MUC5NVc>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-Axl (Y702) / Axl / Cleaved PARP; 

PubMed: 30210917     


H1299 cells were treated with DMSO (NC, negative control), 2.5 μM R428, or 0.5 μM LDC1267 for indicated time periods. Total cell lysates were processed for western blotting analysis using antibodies as indicated.

caspase8 / caspase9 / Bcl-xl / Bcl-2; 

PubMed: 30210917     


Hela cells were treated with DMSO (NC, negative control) or 2.5 μM R428 for indicated time periods. Total cell lysates were processed for western blotting analysis using antibodies as indicated. Casp 8, caspase-8. Casp 9, caspase-9.

30210917
Growth inhibition assay
Cell viability; 

PubMed: 30210917     


Hela cells were treated with DMSO or 2.5 μM R428 in the presence or absence of 10 μM Z-VAD-FMK (ZVAD) for 72 hours. Cell viability was evaluated by MTT assay. **, P<0.01, Student’s T test. Error bars, mean ± SD.

30210917
Immunofluorescence
LAMP1 / Lysosome; 

PubMed: 30210917     


H4-LAMP1-GFP cells were treated with DMSO or 2.5 μM R428 for 24 hr and stained with 50 nM lysosome-tracker red. 2 μg/ml Hoechst was used to stain nucleus. Fixed samples were visualized by confocal microscopy. Magnification: ×600. Yellow arrows indicate the undyed vacuoles.

E-cadherin / Vimentin / Axl; 

PubMed: 26670048     


Representative images showing the expression of E-cadherin, Vimentin, and AXL in MICs (metastatic initiating cells) 24 hr after treatment with DMSO or R428. Scale bar, 20 μm. 

30210917 26670048
In vivo Pharmacologic investigations reveal favorable exposure after oral administration such that R428-treated tumors display a dose-dependent reduction in expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail. In support of an earlier study, R428 inhibits angiogenesis in corneal micropocket and tumor models. R428 administration reduces metastatic burden and extends survival in MDA-MB-231 intracardiac and 4T1 orthotopic (median survival, >80 days compared with 52 days; P < 0.05) mouse models of breast cancer metastasis. [1]

Protocol

Animal Research:

[1]
+ Expand
  • Animal Models: MDA-MB-231-luc-D3H2LN Intracardiac Model
  • Formulation: 0.5% hydroxypropylmethylcellulose + 0.1% Tween 80
  • Dosages: 125 mg/kg
  • Administration: Oral, twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 6 mg/mL warmed (11.84 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing. 		1mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 506.64
Formula

C30H34N8
CAS No. 1037624-75-1
Storage powder
in solvent
Synonyms

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03649321 Recruiting Cancer of Pancreas University of Texas Southwestern Medical Center|Triligent International|Translational Genomics Research Institute|BerGenBio ASA January 3 2019 Phase 1|Phase 2
NCT03649321 Recruiting Cancer of Pancreas University of Texas Southwestern Medical Center|Triligent International|Translational Genomics Research Institute|BerGenBio ASA January 3 2019 Phase 1|Phase 2
NCT02872259 Recruiting Melanoma Haukeland University Hospital|BerGenBio ASA February 13 2017 Phase 1|Phase 2
NCT02872259 Recruiting Melanoma Haukeland University Hospital|BerGenBio ASA February 13 2017 Phase 1|Phase 2
NCT02922777 Recruiting Non-Small Cell Lung Carcinoma University of Texas Southwestern Medical Center|Texas Tech University Health Sciences Center|BerGenBio ASA November 2016 Phase 1
NCT02922777 Recruiting Non-Small Cell Lung Carcinoma University of Texas Southwestern Medical Center|Texas Tech University Health Sciences Center|BerGenBio ASA November 2016 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    Could you please let me know whether this compound is an enantiomer or it is in its racemic form?

  • Answer:

    Our S2841 R428 is S enantiomer, and its e.e. value (enantiomeric purity) >98%.

selleck catalog

TAM Receptor Signaling Pathway Map
Tags: buy R428 (BGB324|Bemcentinib) | R428 (BGB324|Bemcentinib) supplier | purchase R428 (BGB324|Bemcentinib) | R428 (BGB324|Bemcentinib) cost | R428 (BGB324|Bemcentinib) manufacturer | order R428 (BGB324|Bemcentinib) | R428 (BGB324|Bemcentinib) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID