R428 (BGB324)
Catalog No.S2841
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).
7 Customer Reviews
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Flow cytometry analysis showing band 3/α4 integrin expression of luciferase and TET2-knockdown CFU-E cells cultured for 13 days in the presence of DMSO or 0.2 μM R428.
Blood, 2018, doi:10.1182/blood-2018-05-853291. R428 (BGB324) purchased from Selleck.
Cells were treated with R428 at indicated doses for 72-96 hours prior to performing proliferation assays. Proliferation is plotted as a percentage of growth relative to vehicle-treated cells (n=6 in three independent experiments). R428 knockdown of AXL activity was evaluated via IP analysis for pan-tyrosine 24 hours post-treatment.
Clin Cancer Res, 2015, 21(11):2601-12. R428 (BGB324) purchased from Selleck.
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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, 2017, 31(4):1382-1397. R428 (BGB324) purchased from Selleck.
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Time course of pAXL and downstream pAkt detection in the presence of 15μM cisplatin. Phosphorylation of AXL was inhibited by adding 2μM BGB324. Densitometry values as percentage of untreated control are shown for pAXL and pAkt, normalized to respective beta-actin.
Front Pharmacol, 2018, doi:10.3389/fphar.2017.00970. 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.
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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.
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). | ||
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| Targets |
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| 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] |
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| 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: |
+ Expand
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Solubility (25°C)
| In vitro | DMSO | 6 mg/mL warmed (11.84 mM) |
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| 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 |
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| Formula | C30H34N8 |
| CAS No. | 1037624-75-1 |
| Storage | powder |
| in solvent | |
| Synonyms |
Bio Calculators
Molarity Calculator
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Molarity Calculator
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
Could you please let me know whether this compound is an enantiomer or it is in its racemic form?
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Answer:
Our S2841 R428 is S enantiomer, and its e.e. value (enantiomeric purity) >98%.
