Home Protein Tyrosine Kinase Axl inhibitor Bemcentinib (R428) For research use only.

Bemcentinib (R428)

Synonyms: BGB324

Bemcentinib (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).

Bemcentinib (R428) Chemical Structure

Bemcentinib (R428) Chemical Structure

CAS No. 1037624-75-1

Purity & Quality Control

Bemcentinib (R428) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 cells Function assay 24 h concomitant treatment of the cells with R428 and bafilomycin (Baf A1) or alleviated the vacuolization induced by R428. 30210917
Bel7404 cells Function assay 1 μM 48 h R428 altered the lysosomal pH and blocked autophagic degradation. 30210917
H1299 Growth inhibiton assay 48 h R428 inhibited growth of H1299 in a dose-dependent manner with an IC50 of approximately 4 μM. 30210917
LM3 cells Function assay 2.5 μM 0-36 h R428 induced cytoplasmic vacuoles within one hour after R428 treatment, and the vacuoles increased in number and size with time. 30210917
HeLa cells Function assay 1 h Inhibition of recombinant AXL in human HeLa cells after 1 hr by ELISA, IC50=0.03 μM 26555154
KB-8-5-11 Function assay P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen, Potency value= 14.581 μM 31515284
Click to View More Cell Line Experimental Data

Biological Activity

Description Bemcentinib (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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Axl (Y702) / Axl / Cleaved PARP caspase8 / caspase9 / Bcl-xl / Bcl-2 30210917
Growth inhibition assay Cell viability 30210917
Immunofluorescence LAMP1 / Lysosome E-cadherin / Vimentin / Axl 30210917
In Vivo
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]
Animal Research Animal Models MDA-MB-231-luc-D3H2LN Intracardiac Model
Dosages 125 mg/kg
Administration Oral, twice daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03824080 Completed
Acute Myeloid Leukemia|High-risk Myelodysplastic Syndrome|Low-risk Myelodysplastic Syndrome
GWT-TUD GmbH|Groupe Francophone des Myelodysplasies|Amsterdam UMC location VUmc|BerGenBio ASA
 December 20 2018 Phase 2
NCT02922777 Completed
Non-Small Cell Lung Carcinoma
University of Texas Southwestern Medical Center|Texas Tech University Health Sciences Center|BerGenBio ASA
 November 2016 Phase 1
NCT02424617 Completed
Non-Small Cell Lung Cancer
BerGenBio ASA
 March 2015 Phase 1|Phase 2
NCT02488408 Unknown status
Acute Myeloid Leukemia|Myelodysplastic Syndromes
BerGenBio ASA
 September 2014 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 506.64 Formula

C30H34N8
CAS No. 1037624-75-1 SDF Download Bemcentinib (R428) SDF
Smiles C1CCN(C1)C2CCC3=C(CC2)C=C(C=C3)NC4=NN(C(=N4)N)C5=NN=C6C(=C5)CCCC7=CC=CC=C76
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 25 mg/mL ( (49.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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

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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%.

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