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Infigratinib phosphate

Catalog No. T16364   CAS 1310746-10-1
Synonyms: NVP-BGJ398 phosphate, BGJ-398 phosphate

Infigratinib phosphate (BGJ-398 phosphate) is an effective inhibitor of the FGFR family (IC50: 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively).

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Infigratinib phosphate Chemical Structure
Infigratinib phosphate, CAS 1310746-10-1
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Purity: 99.6%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Infigratinib phosphate (BGJ-398 phosphate) is an effective inhibitor of the FGFR family (IC50: 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively).
Targets&IC50 FGFR4:60 nM, FGFR3:1 nM, FGFR1:0.9 nM, FGFR2:1.4 nM
In vitro Infigratinib inhibits the proliferation of the FGFR1-, FGFR2-, and FGFR3-dependent BaF3 cells with IC50 values which are in the low nanomolar range and comparable to those observed for the inhibition of the receptors kinase activity in the enzymatic assay. Infigratinib phosphate suppresses FGFR1, FGFR2, and FGFR3(IC50=~1 nM), FGFR3K650E(IC50=4.9 nM), and FGFR4(IC50=60 nM). IC50 values for all other kinases are in the μM range (FYN, LCK, YES, and ABL, IC50=1.9, 2.5, 1.1, and 2.3 μM, respectively) except for VEGFR2, KIT, and LYN, which are inhibited at submicromolar concentrations (IC50=0.18, 0.75, and 0.3 μM, respectively). Infigratinib (ranging between 1 nM and 10 μM) is effective at inhibiting cell growth of FGFR2-mutant endometrial cancer cells. For the remaining cells, all IC50 values are greater than 1.5 μM except for VEGFR2 (IC50 1449 and 938 nM), for which there is at least a 400-fold selectivity versus FGFR1, FGFR2, and FGFR3[1][2].
In vivo Infigratinib (30 mg/kg) significantly suppresses the growth of FGFR2-mutated endometrial cancer xenograft models. 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. Infigratinib shows a rapid distribution from the vascular compartment into the peripheral tissues after intravenous dosing, translating into a high volume of distribution (26 L/kg). The relevant pharmacokinetic (PK) parameters indicate that the oral bioavailability of Infigratinib in this study is 32%. 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][2].
Synonyms NVP-BGJ398 phosphate, BGJ-398 phosphate
Molecular Weight 658.47
Formula C26H34Cl2N7O7P
CAS No. 1310746-10-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 11.7mg/mL (17.8mM)

TargetMolReferences and Literature

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 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.

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Keywords

Infigratinib phosphate 1310746-10-1 Angiogenesis Tyrosine Kinase/Adaptors FGFR NVP-BGJ398 Phosphate BGJ-398 Phosphate Infigratinib Phosphate BGJ398 Phosphate NVP-BGJ398 phosphate BGJ-398 phosphate BGJ 398 Phosphate NVP-BGJ 398 Phosphate NVP-BGJ-398 Phosphate inhibitor inhibit

 

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