Home Protein Tyrosine Kinase Axl inhibitor Bemcentinib (R428)

Bemcentinib (R428)

Catalog No.S2841 Synonyms: BGB324

For research use only.

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

CAS No. 1037624-75-1

Selleck's Bemcentinib (R428) has been cited by 93 publications

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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

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 M{jVWmZ2dmO2aX;uJIF{e2G7 NWDTc5g1OSCq M1\ZXmlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgRXhNKGmwIHj1cYFvKEinTHGgZ4VtdHNiYX\0[ZIhOSCqcjDifUBGVEmVQTygTWM2OD1yLkCzJO69VQ>? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV3NUG1OEc,OjZ3NUWxOVQ9N2F-
H1299 MnTGS5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? MXe0PEBp NELLZpJTPDJ6IHnubIljcXSnZDDndo94fGhib3[gTFEzQTliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJid3n0bEBidiCLQ{WwJI9nKGGycILvfIlu[XSnbImgOEDPxE1w Mnj0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MUC5NVcoRjNyMkGwPVE4RC:jPh?=
LM3 cells MUDGeY5kfGmxbjDhd5NigQ>? NXG5VYlQOi53IN88US=> Ml3ENE0{PiCq NH\mRWRTPDJ6IHnu[JVk\WRiY4n0c5Bt[XOvaXOgeoFkfW:uZYOge4l1cGmwIH;u[UBpd3W{IHHmeIVzKFJ2MkigeJJm[XSvZX70MEBidmRidHjlJJZi[3WxbHXzJIlv[3KnYYPl[EBqdiCwdX3i[ZIh[W6mIIPpfoUhf2m2aDD0bY1mNg>? M{TXclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkGwPVE4Lz5|MEKxNFkyPzxxYU6=
Bel7404 cells NXjCOWxpTnWwY4Tpc44h[XO|YYm= MVmxJO69VQ>? MmHIOFghcA>? MV;SOFI5KGGudHXy[YQhfGinIHz5d49{d22jbDDwTEBidmRiYnzvZ4tm\CCjdYTvdIhi\2mlIHTl[5Ji\GG2aX;uMi=> MkjTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MUC5NVcoRjNyMkGwPVE4RC:jPh?=
A549 cells NEThd49HfW6ldHnvckBie3OjeR?= MWOyOEBp MYPjc45kd22rdHHueEB1emWjdH3lcpQhd2ZidHjlJINmdGy|IIfpeIghWjR{ODDhcoQh[mGoaXzvcZlkcW5iKFLh[kBCOSlib4KgZ4htd3KxcYXpcoUhMEOTKTDhcIxmfmmjdHXkJJRp\SC4YXP1c4xqgmG2aX;uJIlv\HWlZXSgZpkhWjR{OD6= NVPPTYNqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNVA6OTdpPkOwNlExQTF5PD;hQi=>
KB-8-5-11 NVexSlF5TnWwY4Tpc44h[XO|YYm= MkjGVE1odHmlb4Dyc5RmcW5ic4Xid5Rz[XSnczDp[IVvfGmoaXXkJIlvKEuELUitOU0yOSCjZHXuc4NiemOrbn;tZUBk\WyuIHzpcoUtKHGKVGOgeIhmemGyZYX0bYMhdGmkcnHyfUB{[3KnZX6sJHBwfGWwY4mgeoFtfWV;IEG0MlU5OSEQvF2= MnH4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3MUWyPFQoRjNzNUG1Nlg1RC:jPh?=
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot caspase8 / caspase9 / Bcl-xl / Bcl-2 ; p-Axl (Y702) / Axl / Cleaved PARP 30210917
Growth inhibition assay Cell viability 30210917
Immunofluorescence E-cadherin / Vimentin / Axl ; LAMP1 / Lysosome 26670048 30210917
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 (from reference)

Animal Research:

[1]
  • Animal Models: MDA-MB-231-luc-D3H2LN Intracardiac Model
  • 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 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCN(C1)C2CCC3=C(CC2)C=C(C=C3)NC4=NN(C(=N4)N)C5=NN=C6C(=C5)CCCC7=CC=CC=C76

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03824080 Completed Drug: Bemcentinib Acute Myeloid Leukemia|High-risk Myelodysplastic Syndrome|Low-risk Myelodysplastic Syndrome GWT-TUD GmbH|Groupe Francophone des Myelodysplasies|VU University Medical Center|BerGenBio ASA December 20 2018 Phase 2
NCT02922777 Recruiting Drug: BGB324|Drug: Docetaxel 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 Drug: erlotinib|Drug: bemcentinib Non-Small Cell Lung Cancer BerGenBio ASA March 2015 Phase 1|Phase 2
NCT02488408 Active not recruiting Drug: Bemcentinib|Drug: Cytarabine|Drug: Decitabine Acute Myeloid Leukemia|Myelodysplastic Syndromes BerGenBio ASA September 2014 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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