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NVP BGJ398 phosphate

Product NameNVP BGJ398 phosphate
CAS1310746-10-1
MFC26H34Cl2N7O7P
MW658.47
EINECS
MOL File1310746-10-1.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	insoluble in EtOH; ≥28.07 mg/mL in H2O with gentle warming and ultrasonic; ≥95.7 mg/mL in DMSO
form	Powder
color	White to gray
InChIKey	GUQNHCGYHLSITB-UHFFFAOYSA-N
SMILES	P(O)(O)(O)=O.N(C1C(=C(OC)C=C(OC)C=1Cl)Cl)C(=O)N(C1=NC=NC(NC2C=CC(N3CCN(CC)CC3)=CC=2)=C1)C

Usage And Synthesis

Uses

Infigratinib phosphate (BGJ-398 phosphate; NVP-BGJ398 phosphate) is a potent inhibitor of the FGFR family with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

Biological Activity

ic50 value: 0.9 nm (fgfr1); 1.4 nm (fgfr2); 1 nm (fgfr2) [1] nvp-bgj398 is a novel selective, pan-specific fgfr inhibitor currently in phase i

in vivo

Infigratinib is administered to athymic nude mice implanted subcutaneously with RT112/luc1 tumors: either as a 5 mg/kg intravenous bolus in NMP/PEG200 (1:9, v/v) or orally by gavage as a suspension in PEG300/D5W (2:1, v/v) at a 20 mg/kg dose. The relevant pharmacokinetic (PK) parameters indicate that the oral bioavailability of Infigratinib in this study is 32%. After intravenous dosing, Infigratinib shows a rapid distribution from the vascular compartment into the peripheral tissues, translating into a high volume of distribution (26 L/kg). The plasma clearance is high at 3.3 L/h/kg (61% of liver blood flow). The ratio of tumor to plasma after oral dosing based on AUC is determined to be 10^[1]. Infigratinib (30 mg/kg) significantly inhibits the growth of FGFR2-mutated endometrial cancer xenograft models^[2].

IC 50

FGFR1: 0.9 nM (IC₅₀); FGFR2: 1.4 nM (IC₅₀); FGFR3: 1 nM (IC₅₀); FGFR4: 60 nM (IC₅₀)

References

[1] Guagnano V, 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-me thyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor T DOI:10.1021/jm2006222
[2] Konecny GE, et al. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Mol Cancer Ther. 2013 May;12(5):632-42. DOI:10.1158/1535-7163.MCT-12-0999

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