R428 (BGB324)

Catalog No.S2841

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).

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R428 (BGB324) Chemical Structure

R428 (BGB324) Chemical Structure
Molecular Weight: 506.64

Validation & Quality Control

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Quality Control & MSDS

Related Compound Libraries

R428 (BGB324) is available in the following compound libraries:

Product Information

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  • Research Area
  • Inhibition Profile

Product Description

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]
IC50 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]
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(Only for Reference)

Kinase Assay: [1]

In vitro Kinase Assays A five-point R428 dose titration is performed in radiometric in vitro kinase assays on 133 kinases at the KmATP for each kinase. Axl, Mer, and Tyro3 assays are also performed using a fluorescence polarization protocol. HER2 activity is determined by Z'-LYTE assay.

Animal Study: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Holland SJ, et al. Cancer Res, 2010, 70(4), 1544-1554.

[2] Ghosh AK, et al. Blood, 2011, 117(6), 1928-1937.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02424617 Recruiting Non-Small Cell Lung Cancer BerGenBio AS March 2015 Phase 1|Phase 2
NCT02488408 Recruiting Acute Myeloid Leukemia BerGenBio AS September 2014 Phase 1

Chemical Information

Download R428 (BGB324) SDF
Molecular Weight (MW) 506.64


CAS No. 1037624-75-1
Storage 3 years -20℃powder
2 years -80℃in solvent
Solubility (25°C) * In vitro DMSO 6 mg/mL warming (11.84 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 5% DMSO+corn oil 1mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 1H-1,2,4-Triazole-3,5-diamine, 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl]-

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%.

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.

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