An FGFR inhibitor
Related Products
Alternative(s)
19157BGJ398
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BGJ398 (phosphate)

Item No. 39292

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N′-(2,6-dichloro-3,5-dimethoxyphenyl)-N-[6-[[4-(4-ethyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]-N-methyl-urea, monophosphate
CAS Number
1310746-10-1
Synonyms
  • Infigratinib (phosphate)
  • NVP-BGJ398 (phosphate)
Molecular Formula
C26H31Cl2N7O3 • H3PO4
Formula Weight
658.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly solubleDMSO: Slightly solubleWater: Slightly soluble
SMILES
COC1=C(Cl)C(NC(N(C)C2=CC(NC3=CC=C(N4CCN(CC)CC4)C=C3)=NC=N2)=O)=C(Cl)C(OC)=C1.OP(O)(O)=O
InChi Code
InChI=1S/C26H31Cl2N7O3.H3O4P/c1-5-34-10-12-35(13-11-34)18-8-6-17(7-9-18)31-21-15-22(30-16-29-21)33(2)26(36)32-25-23(27)19(37-3)14-20(38-4)24(25)28;1-5(2,3)4/h6-9,14-16H,5,10-13H2,1-4H3,(H,32,36)(H,29,30,31);(H3,1,2,3,4)
InChi Key
GUQNHCGYHLSITB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    BGJ398 is an orally available inhibitor of human FGFRs (IC50s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).1,2 It inhibits FGFR4 and VEGFR2 with IC50 values of 60 and 180 nM, respectively, and displays comparatively little activity towards Abl, Fyn, Kit, Lck, Lyn, and Yes (IC50s = 0.3-2.5 µM).1 BGJ398 has been shown to suppress the proliferation of cancer cells with wild-type FGFR3 overexpression (IC50s = 5, 30, 32, and 15 nM, for RT112, RT4, SW780, and JMSU1 cells, respectively).1 In an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3, BGJ398 inhibited tumor growth after oral administration of 10-30 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Guagnano, V., Furet, P., Spanka, C., et al. 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. J. Med. Chem. 54(20), 7066-7083 (2011).

    2. Hagel, M., Miduturu, C., Sheets, M., et al. First selective small molecule inhibitor of FGFR4 for the treatment of hepatocellular carcinomas with an activated FGFR4 signaling pathway. Cancer Discov. 5(4), 424-437 (2015).