R428 (BGB324)

Catalog No.S2841

R428 (BGB324) 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).

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4 Customer Reviews

  • Cetuximab-resistant cells are sensitive to therapeutic blockade of AXL activity with the AXL TKI R428. Cells were treated with vehicle (-) or indicated doses of R428 for 24 hours before harvesting whole-cell lysate and immunoblotting for the indicated proteins. α-Tubulin was used as a loading control.

    Cancer Res 2014 74(18), 5152-64. R428 (BGB324) purchased from Selleck.

    B) The processing of AXL is increased by an AXL kinase inhibitor. Panc-28 cells were incubated overnight with DMSO or 150 nM R428, a selective AXL kinase inhibitor, before examining by Western blot the levels of endogenous AXL-FL and AXL-CTF (C-20; left). Levels of AXL-CTF in DAPT-treated cells were quantified as described above and unpaired Student’s t test was employed for the analysis (right). Data are shown as means±SEM (n = 4). ***P<0.001.

    FASEB J, 2016. R428 (BGB324) purchased from Selleck.

  • HCC827-ER cells were divided into four subgroups and treated with 15 μM Erlotinib, 1 μM R428 (a specific AXL inhibitor), 1 μM R428 + 15 μM Erlotinib, and DMEM as a control for 24 h, respectively. Cell viability (A) and apoptosis (B) in HCC827-ER were assessed by MTT and apoptosis assays, respectively. (*P<0.05 vs Control). Expression of the AXL, MAPK, AKT, Survivin and apoptosis pathway-related proteins were assessed by immunoblotting.

    Am J Transl Res, 2016, 8(11):4857-4868. R428 (BGB324) purchased from Selleck.

    Axl inhibitor promotes the apoptosis induced by ALK-TKIs. (A) After treated with crizotinib (100 nM), BGB324 (300 nM) or their combination for 48 h, cell apoptosis was determined by flow cytometry. (B) The induction of apoptosis by ceritinib (100 nM), BGB324 (300 nM) or their combination was examined. (C and D) Cells were treated with crizotinib (100 nM), BGB324 (300 nM) or their combination for 48 h, then whole-cell lysates were collected and the levels of indicated protein were analyzed by Western blot in (C) NB1643 and (D) SHSY5Y cells. *P < 0.05 for the indicated comparisons; ns, not significant.

    Biochem Bioph Res Co 2014 10.1016/j.bbrc.2014.10.126. R428 (BGB324) purchased from Selleck.

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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]
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

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 <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 Information

Molecular Weight 506.64
Formula

C30H34N8

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02872259 Recruiting Melanoma Haukeland University Hospital|BerGenBio AS January 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 AS November 2016 Phase 1
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

Tech Support

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TAM Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID