PEMIGATINIB


Synonyms	Fgfr inhibitor incb054828 INCB054828 Incb-054828 Incb054828 Pemazyre Pemigatinib
Status
Molecule Category	UNKNOWN
ATC	L01EX20
UNII	Y6BX7BL23K


Active Pharmaceutical Ingredients Bioactive chemicals	Exact Similarity SubStructure	Threshold (%) >= 70


InChI Key	HCDMJFOHIXMBOV-UHFFFAOYSA-N
Smiles	CCN1C(=O)N(c2c(F)c(OC)cc(OC)c2F)Cc2cnc3[nH]c(CN4CCOCC4)cc3c21
InChI	InChI=1S/C24H27F2N5O4/c1-4-30-21-14(11-27-23-16(21)9-15(28-23)13-29-5-7-35-8-6-29)12-31(24(30)32)22-19(25)17(33-2)10-18(34-3)20(22)26/h9-11H,4-8,12-13H2,1-3H3,(H,27,28)

Mechanism of Action	Action	Reference
Fibroblast growth factor receptor 1 inhibitor	INHIBITOR	FDA


Protein: Fibroblast growth factor receptor 1 Description: Fibroblast growth factor receptor 1 Organism : Homo sapiens P11362 ENSG00000077782











Protein: Fibroblast growth factor receptor 2 Description: Fibroblast growth factor receptor 2 Organism : Homo sapiens P21802 ENSG00000066468











Protein: Fibroblast growth factor receptor 3 Description: Fibroblast growth factor receptor 3 Organism : Homo sapiens P22607 ENSG00000068078

Assay Description	Organism	Bioactivity
Inhibition of phosphorylated FGFR2alpha in human KATO III stomach cancer cell line spiked in human whole blood incubated for 4 hrs by ELISA	Homo sapiens	11.0 nM
Inhibition of human ERG at 5 uM by patch clamp method relative to control	Homo sapiens	9.0 %
In vivo inhibition of FGFR2 in po dosed SCID mouse xenografted with human KATO III stomach cancer cell line administered as single dose and measured after 4 hrs	Mus musculus	22.0 nM
Inhibition of FGFR1 (unknown origin)	Homo sapiens	0.4 nM
Inhibition of FGFR2 (unknown origin)	Homo sapiens	0.5 nM
Inhibition of FGFR3 (unknown origin)	Homo sapiens	1.2 nM
Inhibition of FGFR4 (unknown origin)	Homo sapiens	30.0 nM

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