R428
Products are for research use only. Not for human use. We do not sell to patients.
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $144.00 | In Stock | 1 | |
| 1mg | $61.00 | In Stock | 1 | |
| 5mg | $130.00 | In Stock | 1 | |
| 10mg | $232.00 | In Stock | 1 | |
| 50mg | $436.00 | In Stock | 1 |
Citations
1 publicationsPublications from researchers using this productDescription
R428, as a Axl inhibitor, blocks Axl autophosphorylation on its C-terminal docking site, Tyr821, at nanomolar concentrations[1].
In vitro, R428 inhibited growth of H1299, a human non-small cell lung carcinoma cell line that had constitutively activated Axl, in a dose-dependent manner with an IC50 of approximately 4 µM[1]. In CE81T cells, the IC50 value of R428 was 1.98 µM when treated for 72 h[2]. In vitro, TNBC cells were treated with 0.5, 1 or 2 µM R428 for 30 min, 1-, 2- and 4-h disrupted the polarized localization of the Golgi apparatus towards the leading edge in migratory cells[3].
In vivo, rats were administrated 100 mg/kg body weight (p.o.) R428 that shown more severe RV hypertrophy, augmented right ventricular systolic pressure (RVSP), impaired cardiac output and worsened tricuspid annular plane systolic excursion, and a significantly increased total pulmonary vascular resistance index[4]. In vivo efficacy test it shown that R428 has a long plasma half-life (13 hours at 75 mg/kg), and distributes effectively to tissue[5].
In vivo, mice (8 weeks of age) were treated with 125 mg/kg R428 orally significantly reduced number of CD4+ T cells in the kidney compared to the T cell numbers in the kidney of nephritic B6 mice[6].
References:
[1] Chen F, et al. Axl inhibitor R428 induces apoptosis of cancer cells by blocking lysosomal acidification and recycling independent of Axl inhibition. Am J Cancer Res. 2018 Aug 1;8(8):1466-1482.
[2] Yang PW, et al. Cabozantinib (XL184) and R428 (BGB324) Inhibit the Growth of Esophageal Squamous Cell Carcinoma (ESCC). Front Oncol. 2019 Nov 6;9:1138.
[3] Zajac O, et al. AXL Controls Directed Migration of Mesenchymal Triple-Negative Breast Cancer Cells. Cells. 2020 Jan 19;9(1):247.
[4] Novoyatleva T, et al. Deficiency of Axl aggravates pulmonary arterial hypertension via BMPR2. Commun Biol. 2021 Aug 24;4(1):1002. doi: 10.1038/s42003-021-02531-1. Erratum in: Commun Biol. 2022 Jan 20;5(1):97.
[5] Zhen Y, et al. Targeted inhibition of Axl receptor tyrosine kinase ameliorates anti-GBM-induced lupus-like nephritis. J Autoimmun. 2018 Sep;93:37-44.
[6] Zhen Y, et al. Axl regulated survival/proliferation network and its therapeutic intervention in mouse models of glomerulonephritis. Arthritis Res Ther. 2022 Dec 28;24(1):284.
Protocol
| Cell experiment [1]: | |
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Cell lines |
B-CPAP cell line(derived from human PTC cancer tissue) |
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Preparation Method |
The B-CPAP cell line was cultured and treated with the AXL inhibitor R428 at different concentrations (0.5 µmol/L, 1 µmol/L, 2 µmol/L, 4 µmol/L), and the untreated B-CPAP cell line was used as a control group. A CCK-8 assay was performed to assess the cell proliferation rate. |
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Reaction Conditions |
0.5 µmol/L, 1 µmol/L, 2 µmol/L, 4 µmol/L; for 24 h |
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Applications |
In the B-CPAP experimental group, the cell survival rates after treatment with 0.5, 1.0, 2.0, and 4.0 µmol/L R428 were 85.28% ± 9.21%, 66.74% ± 3.88%, 41.51% ± 6.33%, and 3.71% ± 2.10%, respectively. |
| Animal experiment [2]: | |
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Animal models |
NOD-SCID male mice |
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Preparation Method |
In the animal model, ESCC (Esophageal squamous cell carcinoma) xenograft models were established by injecting KYSE-70 cells with Matrigel into the upper back region of NOD-SCID male mice followed by treatment with vehicle control, R428 (50 mg/kg/day), cisplatin (1.0 mg/kg), or cabozantinib (30 mg/kg/day) for the indicated number of days. |
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Dosage form |
50 mg/kg/day; i.p. |
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Applications |
R428 alone significantly inhibited ESCC tumor growth compared to the vehicle; however, no synergistic effect with cisplatin was observed. |
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References: [1] Wei M, et al. AXL, along with PROS1, is overexpressed in papillary thyroid carcinoma and regulates its biological behaviour. World J Surg Oncol. 2022 Oct 6;20(1):334. |
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Product Documents
Chemical Properties
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
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