DOVITINIB LACTATE

Details

Stereochemistry	RACEMIC
Molecular Formula	C21H21FN6O.C3H6O3.H2O
Molecular Weight	500.5227
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=QDPVYZNVVQQULH-UHFFFAOYSA-N

InChI=1S/C21H21FN6O.C3H6O3.H2O/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;1-2(4)3(5)6;/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29);2,4H,1H3,(H,5,6);1H2

HIDE SMILES / InChI

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 43 Target ID: CHEMBL1974 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8297	0.001 µM [IC50]
Stem cell growth factor receptor 53 Target ID: CHEMBL1936 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8297	0.002 µM [IC50]
Macrophage colony stimulating factor receptor 24 Target ID: CHEMBL1844 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8297	0.036 µM [IC50]
Fibroblast growth factor receptor 1 45 Target ID: CHEMBL3650 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8297	0.008 µM [IC50]
Fibroblast growth factor receptor 3 32 Target ID: CHEMBL2742 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8297	0.009 µM [IC50]
Vascular endothelial growth factor receptor 1 41 Target ID: CHEMBL1868 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8297	0.01 µM [IC50]
Vascular endothelial growth factor receptor 2 104 Target ID: CHEMBL279 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8297	0.013 µM [IC50]
Vascular endothelial growth factor receptor 3 41 Target ID: CHEMBL1955 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8297	0.008 µM [IC50]
Platelet-derived growth factor receptor alpha 30 Target ID: CHEMBL2007 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8297	0.21 µM [IC50]
Platelet-derived growth factor receptor beta 56 Target ID: CHEMBL1913 Sources: https://www.drugbank.ca/drugs/DB05928	Inhibitor 8297	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 656	DOVITINIB Approved Use Unknown
Endometrial cancer 43 Sources: https://www.clinicaltrials.gov/ct2/show/study/NCT01379534	Primary	Phase II 1132	DOVITINIB Approved Use Unknown
Hepatocellular carcinoma 83 Sources: https://www.clinicaltrials.gov/ct2/show/NCT01232296	Primary	Phase II 1132	DOVITINIB Approved Use Unknown
Gastrointestinal stromal tumor 20 Sources: https://www.clinicaltrials.gov/ct2/show/NCT01440959	Primary	Phase II 1132	DOVITINIB Approved Use Unknown
Adenoid cystic carcinoma 6 Sources: https://www.clinicaltrials.gov/ct2/show/NCT01524692	Primary	Phase II 1132	DOVITINIB Approved Use 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 Page: p.2078	unhealthy, ADULT n = 7 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: https://pubmed.ncbi.nlm.nih.gov/18381947 Page: p.2078	Sources: https://pubmed.ncbi.nlm.nih.gov/18381947 Page: p.2078
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 Page: p.6	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: glioblastoma Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27100354 Page: p.6	DLT: Thrombocytopenia, Alanine aminotransferase increased... Disc. AE: Deep vein thrombosis... Other AEs: GGT increased... Dose limiting toxicities: Thrombocytopenia (grade 3-4, 16.7%) Alanine aminotransferase increased (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 Page: p.6
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 Page: p.6	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27100354 Page: p.6	Other AEs: Alanine aminotransferase increase... Other AEs: Alanine aminotransferase increase (grade 3-4) Sources: https://pubmed.ncbi.nlm.nih.gov/27100354 Page: p.6
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 Page: p.2078	unhealthy, ADULT n = 3 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/18381947 Page: p.2078	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 Page: p.2078
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 n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 Sources: https://pubmed.ncbi.nlm.nih.gov/27100354	DLT: Alanine aminotransferase increased, Neutropenia... Other AEs: WBC decreased, Neutropenia... Dose limiting toxicities: Alanine aminotransferase increased (grade 3-4, 25%) Neutropenia (grade 3-4, 25%) Other AEs: WBC decreased (grade 3-4, 25%) Neutropenia (grade 3-4, 50%) Neutropenia (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 Page: p.6	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: glioblastoma Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27100354 Page: p.6
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 Page: p.6	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: glioblastoma Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27100354 Page: p.6
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 Page: p.6	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: glioblastoma Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27100354 Page: p.6
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 Page: p.6	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: glioblastoma Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27100354 Page: p.6
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 Page: p.6	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/27100354 Page: p.6
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 Page: p.2078	unhealthy, ADULT n = 3 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/18381947 Page: p.2078
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 Page: p.2078	unhealthy, ADULT n = 3 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/18381947 Page: p.2078
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 Page: p.2078	unhealthy, ADULT n = 3 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/18381947 Page: p.2078
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 n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 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 n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 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 n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 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 n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 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 n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 Sources: https://pubmed.ncbi.nlm.nih.gov/27100354

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 781 substrate 1737 inhibitor 1587	inhibitor 1767	inhibitor 1852

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1461 CYP2C8 911 BCRP 699 OATP1B1 788 OATP1B3 706	CYP1A2 1054 FMO3 67 CYP1A1 349	MRP3 53 OATP2B1 6 BCRP 75 UGT1A3 9 P-gp 257 MRP1 48 UGT2B7 14 MRP2 111 CYP1A1 108 PXR 9 CYP1A2 701 OATP1B1 26 CYP2C19 293

Drug as perpetrator

Target	Modality	Activity
CYP2C8 965	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/29956478/	no [IC50 ~363 uM]
CYP2C19 1553	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
CYP2D6 1891	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
CYP3A4 1925	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
MRP1 172	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
MRP2 475	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
OATP1B1 803	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
OATP2B1 126	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
P-gp 1650	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
PXR 46	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
UGT1A3 93	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
UGT2B7 157	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	no
OATP1B3 715	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	weak [IC50 105.2 uM]
OATP1B1 803	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	weak [IC50 76.5 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	weak [Inhibition 20 uM]
CYP3A4 1925	inhibitor 3277	weak [Inhibition 20 uM]
AHR 4	activator 214 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes [EC50 0.609 uM]
BCRP 773	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes [IC50 10.3 uM]
BCRP 773	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes
CYP1A1 218	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes
CYP1A2 1692	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes
MRP3 207	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes
P-gp 1650	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/25521244/	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
FMO3 67	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/29101463/	major
CYP1A1 349	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/29101463/	minor
CYP3A4 1737	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/29101463/	minor
CYP1A2 1054	substrate 3367 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
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
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
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
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	92555	http://www.matrixscientific.com/092555.html
Matrix Scientific	94224	http://www.matrixscientific.com/094224.html
Matrix Scientific	125211	http://www.matrixscientific.com/125211.html
Matrix Scientific	147142	http://www.matrixscientific.com/147142.html
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=
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
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
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
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
mcule	MCULE-4153826439	https://mcule.com/MCULE-4153826439/

PubMed

Title	Date	PubMed
CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma.	2005 Apr 1	15598814
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 Jan 22	19113866
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.	2010 Nov 24	21095574
Comprehensive analysis of kinase inhibitor selectivity.	2011 Oct 30	22037378
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.	2011 Oct 30	22037377
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.	2013 Apr 15	23398362

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.

Name

Type

Language

DOVITINIB LACTATE

Official Name

English

4-Amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one mono 2-hydroxypropanoate hydrate

Systematic Name

English

DOVITINIB LACTATE [USAN]

Common Name

English

CHIR-258 (HYDRATE)

Common Name

English

PROPANOIC ACID, 2-HYDROXY-, COMPD. WITH 4-AMINO-5-FLUORO-3-(6-(4-METHYL-1-PIPERAZINYL)-1H-BENZIMIDAZOL-2-YL)-2(1H)-QUINOLINONE, HYDRATE (1:1:1)

Common Name

English

Dovitinib lactate [WHO-DD]

Common Name

English

DOVITINIB LACTATE HYDRATE [JAN]

Common Name

English

TKI258 (HYDRATE)

Common Name

English

DOVITINIB LACTATE, (±)-

Common Name

English

(±)-DOVITINIB LACTATE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1967