Free shipping on all orders over $ 500

BGJ398 (Infigratinib)

Cat. No. M1840
BGJ398 (Infigratinib) Structure
Synonym:

NVP-BGJ398; Infigratinib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 44  USD44 In stock
10mg USD 60  USD60 In stock
50mg USD 115  USD115 In stock
100mg USD 195  USD195 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

BGJ398 (Infigratinib) 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.

Product Citations
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).
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 560.48
Formula C26H31Cl2N7O3
CAS Number 872511-34-7
Purity >99%
Solubility DMSO 10 mg/mL
Storage at -20°C
References

[1] Gottfried E Konecny, et al. Mol Cancer Ther. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells

[2] Vito Guagnano, et al. Cancer Discov. FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor

[3] Guagnano et al. J Med Chem. 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.

Related FGFR Products
EOC317

EOC317 (ACTB-1003) is an orally available kinase inhibitor that inhibits FGFR1, VEGFR2, and tie-2 with IC50 values of 6,2, and 4 nM, respectively.

PRN1371

PRN1371 is a highly selective and potent inhibitor of FGFR1-4 and CSF1R against FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R IC50 The values are 0.6, 1.3, 4.1, 19.3, and 8.1 nM, respectively.

Alofanib (RPT835)

Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells.

ASP5878

ASP5878 is a novel selective FGFR inhibitor with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3 and 4, respectively.

PF-05231023

PF-05231023 is an FGF21-receptor agonist, it is also a potential treatment for T2DM.

  Catalog
Abmole Inhibitor Catalog




Keywords: BGJ398 (Infigratinib), NVP-BGJ398; Infigratinib supplier, FGFR, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.