DOVITINIB

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C21H21FN6O
Molecular Weight	392.4294
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1CCN(CC1)C2=CC3=C(C=C2)N=C(N3)C4=C(N)C5=C(NC4=O)C=CC=C5F

InChI

InChIKey=PIQCTGMSNWUMAF-UHFFFAOYSA-N

InChI=1S/C21H21FN6O/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29)

HIDE SMILES / InChI

Molecular Formula	C21H21FN6O
Molecular Weight	392.4294
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.drugbank.ca/drugs/DB05928 | https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=488976

Dovitinib is an orally active small molecule that exhibits potent inhibitory activity against multiple receptor tyrosine kinases (RTK) involved in tumor growth and angiogenesis. Dovitinib strongly binds to fibroblast growth factor receptor 3 (FGFR3) and inhibits its phosphorylation, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell death. In addition, this agent may inhibit other members of the RTK superfamily, including the vascular endothelial growth factor receptor; fibroblast growth factor receptor 1; platelet-derived growth factor receptor type 3; FMS-like tyrosine kinase 3; stem cell factor receptor (c-KIT); and colony-stimulating factor receptor 1; this may result in an additional reduction in cellular proliferation and angiogenesis, and the induction of tumor cell apoptosis. There are several ongoing Phase I/III clinical trials for dovitinib.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Tyrosine-protein kinase receptor FLT3 42 Target ID: CHEMBL1974 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8504	0.001 µM [IC50]
Stem cell growth factor receptor 57 Target ID: CHEMBL1936 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8504	0.002 µM [IC50]
Macrophage colony stimulating factor receptor 24 Target ID: CHEMBL1844 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8504	0.036 µM [IC50]
Fibroblast growth factor receptor 1 46 Target ID: CHEMBL3650 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8504	0.008 µM [IC50]
Fibroblast growth factor receptor 3 32 Target ID: CHEMBL2742 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8504	0.009 µM [IC50]
Vascular endothelial growth factor receptor 1 44 Target ID: CHEMBL1868 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8504	0.01 µM [IC50]
Vascular endothelial growth factor receptor 2 112 Target ID: CHEMBL279 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8504	0.013 µM [IC50]
Vascular endothelial growth factor receptor 3 41 Target ID: CHEMBL1955 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8504	0.008 µM [IC50]
Platelet-derived growth factor receptor alpha 33 Target ID: CHEMBL2007 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8504	0.21 µM [IC50]
Platelet-derived growth factor receptor beta 56 Target ID: CHEMBL1913 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8504	0.027 µM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Metastatic renal cell carcinoma 4 Sources: https://www.clinicaltrials.gov/ct2/show/record/NCT01223027	Primary	Phase III 665	DOVITINIB Approved Use Unknown
Endometrial cancer 44 Sources: https://www.clinicaltrials.gov/ct2/show/study/NCT01379534	Primary	Phase II 1147	DOVITINIB Approved Use Unknown
Hepatocellular carcinoma 83 Sources: https://www.clinicaltrials.gov/ct2/show/NCT01232296	Primary	Phase II 1147	DOVITINIB Approved Use Unknown
Gastrointestinal stromal tumor 20 Sources: https://www.clinicaltrials.gov/ct2/show/NCT01440959	Primary	Phase II 1147	DOVITINIB Approved Use Unknown
Adenoid cystic carcinoma 6 Sources: https://www.clinicaltrials.gov/ct2/show/NCT01524692	Primary	Phase II 1147	DOVITINIB Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
213.35 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21976540	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		DOVITINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
326.3 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24691021	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:		DOVITINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
3033.87 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21976540	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		DOVITINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5576.4 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24691021	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:		DOVITINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
13.51 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21976540	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		DOVITINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
4% REVIEW https://www.ncbi.nlm.nih.gov/pubmed/29956478			DOVITINIB plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
125 mg 1 times / day multiple, oral MTD Dose: 125 mg, 1 times / day Route: oral Route: multiple Dose: 125 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18381947	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/18381947	Sources: https://pubmed.ncbi.nlm.nih.gov/18381947
500 mg 1 times / day multiple, oral MTD Dose: 500 mg, 1 times / day Route: oral Route: multiple Dose: 500 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	DLT: Alanine aminotransferase increased, Thrombocytopenia... Disc. AE: Deep vein thrombosis... Other AEs: GGT increased... Dose limiting toxicities: Alanine aminotransferase increased (grade 3-4, 16.7%) Thrombocytopenia (grade 3-4, 16.7%) AEs leading to discontinuation/dose reduction: Deep vein thrombosis (grade 3-4, 16.7%) Other AEs: GGT increased (16.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/27100354
300 mg 1 times / day multiple, oral RP2D Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	Other AEs: Alanine aminotransferase increase... Other AEs: Alanine aminotransferase increase (grade 3-4) Sources: https://pubmed.ncbi.nlm.nih.gov/27100354
175 mg 1 times / day multiple, oral Studied dose Dose: 175 mg, 1 times / day Route: oral Route: multiple Dose: 175 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18381947	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/18381947	DLT: Alkaline phosphatase serum increased, Anorexia... Dose limiting toxicities: Alkaline phosphatase serum increased (grade 3, 33.3%) Anorexia (grade 3, 33.3%) Fatigue (grade 3, 33.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/18381947
400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	DLT: Alanine aminotransferase increased, Neutropenia... Other AEs: Neutropenia, Neutropenia... Dose limiting toxicities: Alanine aminotransferase increased (grade 3-4, 25%) Neutropenia (grade 3-4, 25%) Other AEs: Neutropenia (grade 3-4, 50%) Neutropenia (grade 3-4, 25%) WBC decreased (grade 3-4, 25%) Sources: https://pubmed.ncbi.nlm.nih.gov/27100354

AEs

AE	Significance	Dose	Population
GGT increased	16.7%	500 mg 1 times / day multiple, oral MTD Dose: 500 mg, 1 times / day Route: oral Route: multiple Dose: 500 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354
Alanine aminotransferase increased	grade 3-4, 16.7% DLT	500 mg 1 times / day multiple, oral MTD Dose: 500 mg, 1 times / day Route: oral Route: multiple Dose: 500 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354
Thrombocytopenia	grade 3-4, 16.7% DLT	500 mg 1 times / day multiple, oral MTD Dose: 500 mg, 1 times / day Route: oral Route: multiple Dose: 500 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354
Deep vein thrombosis	grade 3-4, 16.7% Disc. AE	500 mg 1 times / day multiple, oral MTD Dose: 500 mg, 1 times / day Route: oral Route: multiple Dose: 500 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354
Alanine aminotransferase increase	grade 3-4	300 mg 1 times / day multiple, oral RP2D Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354
Anorexia	grade 3, 33.3% DLT	175 mg 1 times / day multiple, oral Studied dose Dose: 175 mg, 1 times / day Route: oral Route: multiple Dose: 175 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18381947	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/18381947
Fatigue	grade 3, 33.3% DLT	175 mg 1 times / day multiple, oral Studied dose Dose: 175 mg, 1 times / day Route: oral Route: multiple Dose: 175 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18381947	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/18381947
Alkaline phosphatase serum increased	grade 3, 33.3% DLT, Disc. AE	175 mg 1 times / day multiple, oral Studied dose Dose: 175 mg, 1 times / day Route: oral Route: multiple Dose: 175 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18381947	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/18381947
Neutropenia	grade 3-4, 25%	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354
WBC decreased	grade 3-4, 25%	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354
Alanine aminotransferase increased	grade 3-4, 25% DLT	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354
Neutropenia	grade 3-4, 25% DLT	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354
Neutropenia	grade 3-4, 50%	400 mg 1 times / day multiple, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27100354

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087 substrate 1946 inhibitor 2252	inhibitor 2438	inhibitor 2507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1741 BCRP 910 OATP1B1 1079 OATP1B3 961 CYP2C8 1057	CYP1A2 1197 FMO3 77 CYP1A1 389	MRP3 83 OATP2B1 6 BCRP 101 UGT1A3 10 P-gp 301 MRP1 74 UGT2B7 14 MRP2 146 CYP1A1 151 PXR 10 CYP1A2 832 OATP1B1 29 CYP2C19 329

Drug as perpetrator

Target	Modality	Activity
CYP2C8 1117	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/29956478/	no [IC50 >=363 uM]
CYP2C19 2141	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
CYP2D6 2546	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
CYP3A4 2633	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
MRP1 232	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
MRP2 625	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
OATP1B1 1095	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
OATP2B1 162	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
P-gp 1932	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
PXR 51	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
UGT1A3 99	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
UGT2B7 210	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
OATP1B3 970	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	weak [IC50 105.2 uM]
OATP1B1 1095	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	weak [IC50 76.5 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	weak [Inhibition 20 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	weak [Inhibition 20 uM]
AHR 9	activator 342 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes [EC50 0.609 uM]
BCRP 985	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes [IC50 10.3 uM]
BCRP 985	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes
CYP1A1 272	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes
CYP1A2 2333	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes
MRP3 326	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
FMO3 77	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/29101463/	major
CYP1A1 389	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/29101463/	minor
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/29101463/	minor
CYP1A2 1197	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/29101463/	minor	yes (co-administration study) Comment: Fluvoxamine increased Cmax and AUC(0-72h) by 80% and 188%. Sources: https://pubmed.ncbi.nlm.nih.gov/29101463/

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY100488	https://www.001chemical.com/chem/search?q=DY100488
001 Chemical	DY113935	https://www.001chemical.com/chem/search?q=DY113935
1PlusChem LLC	1P006NVL	https://www.1pchem.com/search?query=1P006NVL
1PlusChem LLC	1P0077ER	https://www.1pchem.com/search?query=1P0077ER
A2B Chem	AD35395	http://a2bchem.com/prod/AD35395
Aceschem	ACF022913	https://www.aceschem.com/catalog/search.do?q=ACF022913
Aceschem	ACF022914	https://www.aceschem.com/catalog/search.do?q=ACF022914
Aceschem	ACF022915	https://www.aceschem.com/catalog/search.do?q=ACF022915
AChemBlock	M15657	http://www.achemblock.com/catalogsearch/result/?q=M15657
AK Scientific	2386AH	https://aksci.com/item_detail.php?cat=2386AH
AK Scientific	Y0274	https://aksci.com/item_detail.php?cat=Y0274
AK Scientific	Y0345	https://aksci.com/item_detail.php?cat=Y0345
Angene	AGN-PC-0RNYHU	http://www.angenechemical.com/productshow/AGN-PC-0RNYHU.html
Angene	AGN-PC-0TV656	http://www.angenechemical.com/productshow/AGN-PC-0TV656.html
ApexBio Technology	B5953	https://www.apexbt.com/catalogsearch/result/?q=B5953
AstaTech	42194	http://astatechinc.com/CPSResult.php?CRNO=42194
AstaTech	C75053	http://astatechinc.com/CPSResult.php?CRNO=C75053
BLD Pharm	BD216013	http://www.bldpharm.com/search/Search.html?keyword=BD216013
BLD Pharm	BD93948	http://www.bldpharm.com/search/Search.html?keyword=BD93948
BOC Sciences	405169-16-6	http://www.bocsci.com/description.asp?cas=405169-16-6
BOC Sciences	692737-80-7	http://www.bocsci.com/description.asp?cas=692737-80-7
BOC Sciences	915769-50-5	http://www.bocsci.com/description.asp?cas=915769-50-5
Cayman Chemical	15220	http://www.caymanchem.com/app/template/Product.vm/catalog/15220
Chem Scene	CS-0120	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0120
Chem Scene	CS-6230	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-6230
ChemShuttle	111610	https://www.chemshuttle.com/catalogsearch/result/?q=111610
ChemShuttle	111611	https://www.chemshuttle.com/catalogsearch/result/?q=111611
ChemShuttle	112898	https://www.chemshuttle.com/catalogsearch/result/?q=112898
ChemShuttle	141616	https://www.chemshuttle.com/catalogsearch/result/?q=141616
Combi-Blocks	QJ-9735	http://www.combi-blocks.com/cgi-bin/find.cgi?QJ-9735
eMolecules	31230347	https://orderbb.emolecules.com/search/#?query=31230347
eMolecules	37153221	https://orderbb.emolecules.com/search/#?query=37153221
eMolecules	44152097	https://orderbb.emolecules.com/search/#?query=44152097
eMolecules	44455460	https://orderbb.emolecules.com/search/#?query=44455460
eMolecules	72979988	https://orderbb.emolecules.com/search/#?query=72979988
eNovation Chemicals	D372085	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D372085&searchbtn.x=0&searchbtn.y=0
eNovation Chemicals	D395233	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D395233&searchbtn.x=0&searchbtn.y=0
Excenen	EX-A2051	http://www.excenen.com/searchresultlist.php?id=EX-A2051
Exclusive Chemistry	2257	http://www.exchemistry.com/chem-catalog/product-2257.html
Hairui	HR115405	http://www.hairuichem.com/en/product/search.do?q=HR115405
KeyOrganics	AS-19556	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-19556
Lab Network	LN01328149	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01328149
Matrix Scientific	125211	http://www.matrixscientific.com/125211.html
Matrix Scientific	147142	http://www.matrixscientific.com/147142.html
Matrix Scientific	92555	http://www.matrixscientific.com/092555.html
Matrix Scientific	94224	http://www.matrixscientific.com/094224.html
mcule	MCULE-4153826439	https://mcule.com/MCULE-4153826439/
MedChem Express	HY-10207	https://www.medchemexpress.com/search.html?q=HY-10207&ft=&fa=&fp=
MedChem Express	HY-50905	https://www.medchemexpress.com/search.html?q=HY-50905&ft=&fa=&fp=
Molcore	MC100488	http://www.molcore.com/CatMC100488.html
Molcore	MC113935	http://www.molcore.com/CatMC113935.html
Molnova	M15649	https://www.molnova.com/en/serch-list.html?keywords=M15649
MolPort	MolPort-009-679-406	https://www.molport.com/shop/molecule-link/MolPort-009-679-406
MolPort	MolPort-021-783-238	https://www.molport.com/shop/molecule-link/MolPort-021-783-238
MolPort	MolPort-023-279-417	https://www.molport.com/shop/molecule-link/MolPort-023-279-417
Selleck Chemicals	S2769	http://www.selleckchem.com/search.html?searchDTO.searchParam=S2769
Selleck Chemicals	S7765	http://www.selleckchem.com/search.html?searchDTO.searchParam=S7765
ShangHai Biochempartner	BCP000219	http://www.biochempartner.com/search_BCP000219
ShangHai Biochempartner	BCP01981	http://www.biochempartner.com/search_BCP01981
ShangHai Biochempartner	BCP04112	http://www.biochempartner.com/search_BCP04112
ShangHai Biochempartner	BCP11139	http://www.biochempartner.com/search_BCP11139
ShangHai Biochempartner	BCP27905	http://www.biochempartner.com/search_BCP27905
Synovel	SN-0460	http://www.synovellab.com/?s=SN-0460&submit=Search
Synthonix	14560	https://synthonix.com/catalogsearch/result/?q=14560
Tetrahedron	TS86312	http://www.thsci.com/search.do?q=TS86312
Toronto Research Chemicals	B689927	https://www.trc-canada.com/product-detail/?CatNum=B689927

PubMed

Title	Date	PubMed
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.	2013-04-15	23398362
Comprehensive analysis of kinase inhibitor selectivity.	2011-10-30	22037378
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.	2011-10-30	22037377
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.	2010-11-24	21095574
Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.	2009-01-22	19113866
CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma.	2005-04-01	15598814

Patents

Sample Use Guides

In Vivo Use Guide

Patients received 500 mg of dovitinib taken orally on 5 days on/2 days off dosing schedule.

Route of Administration: Oral

In Vitro Use Guide

Dovitinib (CHIR-258) inhibited members of the class III receptor tyrosine kinases (RTK) including FLT3, c-Kit, CSF-1R, and PDGFRa/b with IC50 values of 0.001 to 0.21 mM as assessed by in vitro kinase assays. In addition, CHIR-258 potently inhibited class IV (FGFR1 and 3) and class V (VEGFR1-4) RTKs with IC50 values of 0.008 to 0.013 mM. For insulin receptor, EGFR, c-Met, EphrinA2, Tie2, IGFR1, and HER2 significant inhibition was observed only at more than 10-fold higher concentrations. These studies demonstrated that CHIR-258 is a selective but multitargeted inhibitor of class III, IV, and V RTKs with high potency against FGFRs.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:24:57 GMT 2025` Edited by `admin` on `Mon Mar 31 18:24:57 GMT 2025`
Record UNII	I35H55G906
Record Status	`Validated (UNII)`
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Name

Type

Language

DOVITINIB

Official Name

English

GFKI-258

Preferred Name

English

Dovitinib [WHO-DD]

Common Name

English

TKI-258

Code

English

4-AMINO-5-FLUORO-3-(6-(4-METHYLPIPERAZIN-1-YL)-1H-BENZIMIDAZOL-2-YL)QUINOLIN-2(1H)-ONE

Systematic Name

English

dovitinib [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C129825