NVP BGJ398 phosphate
NVP BGJ398 phosphate Basic information
- Product Name:
- NVP BGJ398 phosphate
- Synonyms:
-
- INFIGRATINIB PHOSPHATE;BGJ-398 PHOSPHATE
- BGJ-398 PHOSPHATE; BGJ 398 PHOSPHATE; NVP BGJ398 PHOSPHATE
- BGJ 398 phosphate
- BGJ-398 phosphate
- NVP BGJ398 phosphate
- NVP-BGJ398 (phosphate)
- N'-(2,6-Dichloro-3,5-dimethoxyphenyl)-N-[6-[[4-(4-ethyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]-N-methylurea phosphate (1:1)
- BGJ-398,NVP-BGJ398,Infigratinib
- CAS:
- 1310746-10-1
- MF:
- C26H34Cl2N7O7P
- MW:
- 658.47
- Mol File:
- 1310746-10-1.mol
NVP BGJ398 phosphate 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
NVP BGJ398 phosphate 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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