Compound Detail

CHEMBL1834657

INFIGRATINIB PHOSPHATE

💊 Approved Drug

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💊 Approved Drug

CCN1CCN(c2ccc(Nc3cc(N(C)C(=O)Nc4c(Cl)c(OC)cc(OC)c4Cl)ncn3)cc2)CC1.O=P(O)(O)O

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL1834657
Name	INFIGRATINIB PHOSPHATE
Phase	Approved
Structure Type	MOL
InChI Key	GUQNHCGYHLSITB-UHFFFAOYSA-N
Therapeutic	✓ Yes
Parent Compound	CHEMBL1852688
Active Moiety	CHEMBL1852688

Known Names

BGJ-398 phosphate Infigratinib monophosphate Infigratinib phosphate Truseltiq

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Mechanisms

Molecular Properties

560.5

MW (Da)

5.35

ALogP

HBA

HBD

95.1

PSA (Å²)

0.38

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
First Approval	2021
Availability	Discontinued
Chirality	Achiral

Routes of Administration

Oral

USAN Stem	-tinib
USAN Year	2019

Extended Properties

Molecular Formula	C26H34Cl2N7O7P
MW	658.48
Aromatic Rings	3
Heavy Atoms	38
NP-Likeness	-1.26

Mechanism of Action

Mechanism	Action Type	Target	Direct	Efficacy
Fibroblast growth factor receptor inhibitor	INHIBITOR	Fibroblast growth factor receptor	✓	✓

Indications

Cholangiocarcinoma Cholangiocarcinoma Neoplasms

Activity Summary

IC50 55 meas. best 9.15

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Fibroblast growth factor receptor 3 CHEMBL2742	IC50	9.15	8.4175	0.7	8
Fibroblast growth factor receptor 1 CHEMBL3650	IC50	9.05	8.6433	0.9	3
Fibroblast growth factor receptor 2 CHEMBL4142	IC50	8.85	8.62	1.4	3
BaF3 CHEMBL614524	IC50	8.7	7.215	2.0	2
RT-112 CHEMBL614145	IC50	8.3	8.3	5.0	1
NON-PROTEIN TARGET CHEMBL3879801	IC50	7.82	7.82	15.0	1
RT-4 CHEMBL614884	IC50	7.52	7.52	30.0	1
SW780 CHEMBL1075595	IC50	7.5	7.5	32.0	1
Fibroblast growth factor receptor 4 CHEMBL3973	IC50	7.22	7.0	60.0	2
Vascular endothelial growth factor receptor 2 CHEMBL279	IC50	6.75	6.2067	180.0	3
Tyrosine-protein kinase Lyn CHEMBL3905	IC50	6.52	6.02	300.0	2
Mast/stem cell growth factor receptor Kit CHEMBL1936	IC50	6.12	5.86	750.0	2
Tyrosine-protein kinase Yes CHEMBL2073	IC50	5.96	5.96	1100.0	1
HT1197 CHEMBL614836	IC50	5.94	5.94	1157.0	1
Vascular endothelial growth factor receptor 1 CHEMBL1868	IC50	5.82	5.82	1510.0	1
Tyrosine-protein kinase Fyn CHEMBL1841	IC50	5.72	5.72	1900.0	1
Angiopoietin-1 receptor CHEMBL4128	IC50	5.69	5.69	2051.0	1
Vascular endothelial growth factor receptor 3 CHEMBL1955	IC50	5.68	5.68	2072.0	1
Unchecked CHEMBL612545	IC50	5.66	5.635	2192.0	2
Tyrosine-protein kinase ABL1 CHEMBL1862	IC50	5.64	5.64	2300.0	1
Tyrosine-protein kinase Lck CHEMBL258	IC50	5.6	5.6	2500.0	1
Platelet-derived growth factor receptor alpha CHEMBL2007	IC50	5.57	5.57	2718.0	1
Macrophage-stimulating protein receptor CHEMBL2689	IC50	5.54	5.54	2891.0	1
Tyrosine-protein kinase JAK2 CHEMBL2971	IC50	5.54	5.54	2882.0	1
Proto-oncogene tyrosine-protein kinase Src CHEMBL267	IC50	5.53	5.53	2969.0	1
Hepatocyte growth factor receptor CHEMBL3717	IC50	5.52	5.52	3011.0	1
Ephrin type-B receptor 1 CHEMBL5072	IC50	5.52	5.52	3039.0	1
ALK tyrosine kinase receptor CHEMBL4247	IC50	5.51	5.51	3078.0	1
BDNF/NT-3 growth factors receptor CHEMBL4898	IC50	5.5	5.5	3139.0	1
Proto-oncogene tyrosine-protein kinase ROS CHEMBL5568	IC50	5.49	5.49	3263.0	1
Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974	IC50	5.49	5.49	3252.0	1
Non-receptor tyrosine-protein kinase TYK2 CHEMBL3553	IC50	5.48	5.48	3303.0	1
Cytoplasmic tyrosine-protein kinase BMX CHEMBL3834	IC50	5.47	5.47	3405.0	1
Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041	IC50	5.47	5.47	3352.0	1
Insulin receptor CHEMBL1981	IC50	5.47	5.47	3371.0	1
Serine/threonine-protein kinase B-raf CHEMBL5145	IC50	5.38	5.38	4142.0	1
Tyrosine-protein kinase SYK CHEMBL2599	IC50	5.27	5.27	5358.0	1

Pharmacokinetic Data

Parameter	Value	Units	Species
CL	60.0	mL.min-1.kg-1	Rattus norvegicus
CL	55.0	mL.min-1.kg-1	Mus musculus
Cmax	260.0	nM	Rattus norvegicus
Cmax	970.0	nM	Rattus norvegicus
Cmax	1.63	nmol/g	Mus musculus
Cmax	420.0	nM	Mus musculus
Cmax	1.68	nmol/g	Mus musculus
Cmax	860.0	nM	Mus musculus
F	51.0	%	Rattus norvegicus
F	32.0	%	Mus musculus
T1/2	4.8	hr	Rattus norvegicus
T1/2	4.5	hr	Rattus norvegicus
T1/2	13.0	hr	Mus musculus
T1/2	4.3	hr	Mus musculus
T1/2	6.7	hr	Mus musculus
T1/2	9.3	hr	Mus musculus
Tmax	4.0	hr	Rattus norvegicus
Tmax	8.0	hr	Mus musculus
Tmax	1.0	hr	Mus musculus
Tmax	2.0	hr	Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Fibroblast growth factor receptor 3	IC50	=	0.7	nM	9.15	Inhibition of FGFR3 juxtamembrane domain-mediated proliferation of mouse BAF3 ce...	21936542
Fibroblast growth factor receptor 1	IC50	=	0.9	nM	9.05	Inhibition of recombinant FGFR1	21936542
Fibroblast growth factor receptor 3	IC50	=	1.0	nM	9.0	Inhibition of recombinant FGFR3	21936542
Fibroblast growth factor receptor 2	IC50	=	1.4	nM	8.85	Inhibition of recombinant FGFR2	21936542
Fibroblast growth factor receptor 3	IC50	=	2.0	nM	8.7	Inhibition of FGFR3-mediated proliferation of mouse BAF3 cells transformed with ...	21936542
Fibroblast growth factor receptor 2	IC50	=	2.0	nM	8.7	Inhibition of FGFR2 juxtamembrane domain-mediated proliferation of mouse BAF3 ce...	21936542
BaF3	IC50	=	2.0	nM	8.7	Antiproliferative activity against mouse BAF3 cell line transformed with TEL-FGF...	21936542
Fibroblast growth factor receptor 1	IC50	=	2.9	nM	8.54	Inhibition of FGFR1-mediated proliferation of mouse BAF3 cells transformed with ...	21936542
Fibroblast growth factor receptor 1	IC50	=	4.6	nM	8.34	Inhibition of wild type FGFR1 expressed in HEK293 cells assessed as inhibition o...	21936542
Fibroblast growth factor receptor 3	IC50	=	4.9	nM	8.31	Inhibition of recombinant FGFR3 K650E mutant	21936542
Fibroblast growth factor receptor 2	IC50	=	4.9	nM	8.31	Inhibition of wild type FGFR2 expressed in HEK293 cells assessed as inhibition o...	21936542
RT-112	IC50	=	5.0	nM	8.3	Antiproliferative activity against human RT112 cells overexpressing wild type FG...	21936542
Fibroblast growth factor receptor 3	IC50	=	5.0	nM	8.3	Inhibition of FGFR3 S249C mutant expressed in HEK293 cells assessed as inhibitio...	21936542
Fibroblast growth factor receptor 3	IC50	=	5.0	nM	8.3	Inhibition of FGFR3 K650E mutant expressed in HEK293 cells assessed as inhibitio...	21936542
Fibroblast growth factor receptor 3	IC50	=	5.0	nM	8.3	Inhibition of GST-fusion FGFR3 K650E mutant using [gamma33P]ATP as substrate aft...	21936542
NON-PROTEIN TARGET	IC50	=	15.0	nM	7.82	Antiproliferative activity against human JMSU1 cells overexpressing wild type FG...	21936542
RT-4	IC50	=	30.0	nM	7.52	Antiproliferative activity against human RT4 cells overexpressing wild type FGFR...	21936542
SW780	IC50	=	32.0	nM	7.5	Antiproliferative activity against human SW780 cells overexpressing wild type FG...	21936542
Fibroblast growth factor receptor 3	IC50	=	52.2	nM	7.28	Inhibition of FGFR3 K650E mutant-mediated proliferation of mouse BAF3 cells tran...	21936542
Fibroblast growth factor receptor 4	IC50	=	60.0	nM	7.22	Inhibition of recombinant FGFR4	21936542

Literature References

PubMed	DOI	Target Context	# Activities
21936542	10.1021/jm2006222	Rattus norvegicus	23
21936542	10.1021/jm2006222	Unchecked	10
21936542	10.1021/jm2006222	Mus musculus	8
21936542	10.1021/jm2006222	Fibroblast growth factor receptor 3	8
21936542	10.1021/jm2006222	Tumor	8
21936542	10.1021/jm2006222	Plasma	8
21936542	10.1021/jm2006222	Tumour	8
21936542	10.1021/jm2006222	RT-112	6
21936542	10.1021/jm2006222	Fibroblast growth factor receptor 1	3
21936542	10.1021/jm2006222	Fibroblast growth factor receptor 2	3
21936542	10.1021/jm2006222	Vascular endothelial growth factor receptor 2	3
21936542	10.1021/jm2006222	Platelet-derived growth factor receptor alpha	2
21936542	10.1021/jm2006222	Receptor-type tyrosine-protein kinase FLT3	2
21936542	10.1021/jm2006222	Hepatocyte growth factor receptor	2
21936542	10.1021/jm2006222	Insulin receptor	2
21936542	10.1021/jm2006222	Fibroblast growth factor receptor 4	2
21936542	10.1021/jm2006222	Tyrosine-protein kinase JAK2	2
21936542	10.1021/jm2006222	Mast/stem cell growth factor receptor Kit	2
21936542	10.1021/jm2006222	ALK tyrosine kinase receptor	2
21936542	10.1021/jm2006222	Tyrosine-protein kinase Lyn	2

Data from ChEMBL 36 via Core Engine