Infigratinib Chemical Properties

Melting point:

>211°C (dec.)

Boiling point:

747.9±60.0 °C(Predicted)

Density 

1.354

storage temp. 

-20°C

solubility 

Soluble in DMSO (up to 5 mg/ml)

form 

White solid.

pka

11.02±0.70(Predicted)

color 

White

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

Infigratinib Usage And Synthesis

Uses

BGJ 398 is a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Description

NVP-BGJ398 (872511-34-7) is a potent and selective pan-FGFR inhibitor (IC50?= 0.9nM, 1.4 nM, 1.0 nM, and 60 nM for FGFR1,2,3,4 respectively).1? It has also been used in a mouse model of Achondroplasia (most common form of dwarfism) to correct pathological hallmarks of this condition.

Uses

BGJ 398 is a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Definition

ChEBI: BGJ-398 is a member of the class of phenylureas that is urea in which a hydrogen attached to one of the nitrogens is replaced by a 2,6-dichloro-3,5-dimethoxyphenyl group, while the hydrogens attached to the other nitrogen are replaced by a methyl group and a 6-{[4-(4-ethylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl group. It is a potent and selective fibroblast growth factor receptor inhibitor. It has a role as a fibroblast growth factor receptor antagonist and an antineoplastic agent. It is an aminopyrimidine, a N-arylpiperazine, a N-alkylpiperazine, a dichlorobenzene and a member of phenylureas.

brand name

Truseltiq

General Description

Class: receptor tyrosine kinase; Treatment: cholangiocarcinoma; Other name: NVP-BGJ398; Elimination half-life = 34 h; Protein binding = 96.8%

target

FGFR1

IC 50

FGFR1~4 IC50 = 0.9, 1.4, 1.0, and 60 nM; VEGFR2 IC50 = 180 nM

References

1) Guagnano?et al.?(2011),?Discovery of 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-{[4-(4-ethyl-1-piperazinyl)phenyl]amino}-4-pyrimidinyl)-1-methylurea (NVP-BGJ398),?a Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase?; J. Med. Chem.?54?7066 2) Komla-Ebri?et al.?(2016),?Tyrosine kinase inhibitor NVP-BGJ398 functionally improves FGFR3-related dwarfism in mouse model; J. Clin. Invest.?126?1871

Infigratinib(872511-34-7)Related Product Information

• PD 173074
• Luminespib
• NVP-BVU 972
• NVP-BEZ 235
• Urease inhibitor
• Recombinant Human Fibroblast Growth Factor Receptor-4 Fc Chimera
• Recombinant Human Fibroblast Growth Factor Receptor-2 Fc Chimera
• Veliparib
• ABT-199
• LMI070
• N-(3-Bromo-4-methylphenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine
• NVS-PAK1-1
• NVP-BSK805
• NVP BGJ398 phosphate
• 3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide
• AZD-4547
• Bortezomib
• NVP-TAE684