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BGJ398

Cat. No. M1840
BGJ398 Structure
Synonym:

NVP-BGJ398

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 120 In stock
50mg USD 220 In stock
200mg USD 580 In stock
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Quality Control
Biological Activity

BGJ398 is a potent and selective FGFR kinase inhibitor with IC50 values of 0.9 nM, 1.4 nM, 1 nM and 60 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. BGJ398 selectively binds to and inhibits the activities of FGFRs, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. FGFRs are a family of receptor tyrosine kinases which may be upregulated in various tumor cell types and may be involved in tumor cell differentiation and proliferation, tumor angiogenesis, and tumor cell survival. BGJ398 significantly decreases the levels of pFRS2 and pMAPK in a dose-dependent manner. BGJ398 does not impair VEGF-induced blood vessel formation. In contrast, BGJ398 inhibits significantly bFGF-stimulated angiogenesis in a dose-dependent manner.

Protocol
Cell Experiment
Cell lines MFE280, SPAC1L, MFE319 cell lines
Preparation method Proliferation assays Cells were plated into 24-well tissue culture plates at a density of 2 × 105 to 5 × 105 and grown without or with increasing concentrations of dovitinib or NVP-BGJ398 (ranging between 0.001 and 10 μmol/L). Cells were harvested by trypsinization on day 7 and counted using a particle counter (Z1; Beckman Coulter Inc.). Experiments were carried out at least 3 times in duplicate for each cell line. Growth inhibition (GI) was calculated as a function of the number of generations. As such, the percentage inhibition was calculated as 1− (cell count divided by cell count of untreated controls). The log of the fractional GI was then plotted against the log of the drug concentration, and the IC50 values were interpolated from the resulting linear regression curve fit (CalcuSyn; Biosoft).
Concentrations 0.001 ~ 10 Μm
Incubation time 7 days
Animal Experiment
Animal models athymic mouse model of endometrial cancer xenografts
Formulation 6 mg in 0.5 mL PEG300 and 0.5 mL acetic acid/acetate buffer, pH 4.68
Dosages 30 mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 560.48
Formula C26H31Cl2N7O3
CAS Number 872511-34-7
Purity 100.00%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Clin Cancer Res (2015). Figure 1.BGJ398
Method Clonogenic or anchorage-independent growth assays
Cell Lines HNSCC cell
Concentrations 1 μM
Incubation Time 24 hrs
Results The full panel of HNSCC cell lines ranking from the most to the least sensitivity to BGJ398 as determined by inhibition of cell proliferation is shown in Fig. 2C and reveals a correlation of TKI sensitivity with the expression of FGFR1 mRNA (p=0.04) and protein p=0.0002).
Rating
References

Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.
Guagnano et al. J Med Chem. 2011 Oct 27;54(20):7066-83. PMID: 21936542.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BGJ398, NVP-BGJ398 supplier, VEGFR/PDGFR, inhibitors

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