U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C20H15ClN4
Molecular Weight 346.813
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of VATALANIB

SMILES

ClC1=CC=C(NC2=C3C=CC=CC3=C(CC4=CC=NC=C4)N=N2)C=C1

InChI

InChIKey=YCOYDOIWSSHVCK-UHFFFAOYSA-N
InChI=1S/C20H15ClN4/c21-15-5-7-16(8-6-15)23-20-18-4-2-1-3-17(18)19(24-25-20)13-14-9-11-22-12-10-14/h1-12H,13H2,(H,23,25)

HIDE SMILES / InChI
Molecular Formula C20H15ClN4
Molecular Weight 346.813
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including: http://www.drugbank.ca/drugs/DB04879 https://en.wikipedia.org/wiki/Vatalanib

Vatalanib a potent oral tyrosine kinase inhibitor with a selective range of molecular targets, has been extensively investigated and has shown promising results in patients with solid tumors in early trials. Vatalanib selectively inhibits the tyrosine kinase domains of vascular endothelial growth factor (VEGF) receptor tyrosine kinases (important enzymes in the formation of new blood vessels that contribute to tumor growth and metastasis), platelet-derived growth factor (PDGF) receptor, and c-KIT. The adverse effects of vatalanib appear similar to those of other VEGF inhibitors. In the CONFIRM trials, the most common side effects were high blood pressure, gastrointestinal upset (diarrhea, nausea, and vomiting), fatigue, and dizziness.

CNS Activity

CNS Penetrant
2588
Sources: DOI: 10.1007/s11224-011-9741-z

Originator

Approval Year

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
 77.0 nM [IC50]
Inhibitor
8504
 37.0 nM [IC50]
Inhibitor
8504
 660.0 nM [IC50]
Inhibitor
8504
 730.0 nM [IC50]
Inhibitor
8504
 580.0 nM [IC50]
Inhibitor
8504
 1.4 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase III
665
Unknown

Approved Use

Unknown
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
3326 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22252616/
500 mg 2 times / day steady-state, oral
dose: 500 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VATALANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2402 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/24838014
1250 mg 1 times / day steady-state, oral
dose: 1250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VATALANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
20391 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22252616/
500 mg 2 times / day steady-state, oral
dose: 500 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VATALANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
23.3 mg × h/L
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/24838014
1250 mg 1 times / day steady-state, oral
dose: 1250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VATALANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
52.9 mg × h/L
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/24838014
1250 mg single, oral
dose: 1250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VATALANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.56 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22252616/
500 mg 2 times / day steady-state, oral
dose: 500 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VATALANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3.8 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/24838014
1250 mg 1 times / day steady-state, oral
dose: 1250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VATALANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
2%
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4243874/
VATALANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
Other AEs: nausea, emesis...
Other AEs:
nausea (6.5%)
emesis (9.7%)
hypertension (6.5%)
Anorexia (3.2%)
Asthenia (6.5%)
Fatigue (6.5%)
lethargy (3.2%)
dizziness (3.2%)
eructation (3.2%)
hyperbilirubinemia (3.2%)
Proteinuria (3.2%)
rash (3.2%)
thrombocytopenia (3.2%)
elevated transaminases (3.2%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
1000 mg 2 times / day multiple, oral
Studied dose
Dose: 1000 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1000 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
DLT: Lethargy, hypertension...
Dose limiting toxicities:
Lethargy (1 pt)
hypertension (1 pt)
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
1000 mg 2 times / day multiple, oral
Studied dose
Dose: 1000 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1000 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
DLT: Nausea, emesis...
Dose limiting toxicities:
Nausea (3 patients)
emesis (2 patients)
Anorexia (1 pt)
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
AEs

AEs

AESignificanceDosePopulation
Anorexia 3.2%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
Proteinuria 3.2%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
dizziness 3.2%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
elevated transaminases 3.2%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
eructation 3.2%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
hyperbilirubinemia 3.2%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
lethargy 3.2%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
rash 3.2%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
thrombocytopenia 3.2%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
Asthenia 6.5%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
Fatigue 6.5%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
hypertension 6.5%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
nausea 6.5%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
emesis 9.7%
750 mg 2 times / day multiple, oral
MTD
Dose: 750 mg, 2 times / day
Route: oral
Route: multiple
Dose: 750 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
Lethargy 1 pt
DLT
1000 mg 2 times / day multiple, oral
Studied dose
Dose: 1000 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1000 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
hypertension 1 pt
DLT
1000 mg 2 times / day multiple, oral
Studied dose
Dose: 1000 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1000 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
Anorexia 1 pt
DLT
1000 mg 2 times / day multiple, oral
Studied dose
Dose: 1000 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1000 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
emesis 2 patients
DLT
1000 mg 2 times / day multiple, oral
Studied dose
Dose: 1000 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1000 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
Nausea 3 patients
DLT
1000 mg 2 times / day multiple, oral
Studied dose
Dose: 1000 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1000 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/16617323
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
DY110757
https://www.001chemical.com/chem/search?q=DY110757
1PlusChem LLC
1P006Z1G
https://www.1pchem.com/search?query=1P006Z1G
1PlusChem LLC
1P00BFLU
https://www.1pchem.com/search?query=1P00BFLU
A2B Chem
AD24548
http://a2bchem.com/prod/AD24548
A2B Chem
AF32642
http://a2bchem.com/prod/AF32642
AA Blocks
AA00BF2E
http://aablocks.com/goods/Goods/detail?id=AA00BF2E
AbovChem LLC
HY-10203
http://www.abovchem.com/pc/en/product_list.aspx?wd=HY-10203
AChemBlock
Q65745
http://www.achemblock.com/catalogsearch/result/?q=Q65745
Achemo Scientific Limited
AC-62276
http://www.achemo.com/search/?Keyword=AC-62276
AK Scientific
0818AB
https://aksci.com/item_detail.php?cat=0818AB
AK Scientific
V0126
https://aksci.com/item_detail.php?cat=V0126
AK Scientific
X6313
https://aksci.com/item_detail.php?cat=X6313
Angene
AGN-PC-088NIF
http://www.angenechemical.com/productshow/AGN-PC-088NIF.html
ApexBio Technology
A1778
https://www.apexbt.com/catalogsearch/result/?q=A1778
ApexBio Technology
A3969
https://www.apexbt.com/catalogsearch/result/?q=A3969
Apollo Scientific
BIFK0006
http://www.apolloscientific.co.uk/chemical_results.php?qstext=BIFK0006&product_group=%25&search_fieldname=header_search
Apollo Scientific
BIFK0044
http://www.apolloscientific.co.uk/chemical_results.php?qstext=BIFK0044&product_group=%25&search_fieldname=header_search
AstaTech
41157
http://astatechinc.com/CPSResult.php?CRNO=41157
AstaTech
41164
http://astatechinc.com/CPSResult.php?CRNO=41164
AstaTech
41169
http://astatechinc.com/CPSResult.php?CRNO=41169
Axon MedChem
1637
https://www.axonmedchem.com/product/1637
BLD Pharm
BD156379
http://www.bldpharm.com/search/Search.html?keyword=BD156379
BLD Pharm
BD169846
http://www.bldpharm.com/search/Search.html?keyword=BD169846
BLD Pharm
BD41450
http://www.bldpharm.com/search/Search.html?keyword=BD41450
BOC Sciences
212141-51-0
http://www.bocsci.com/description.asp?cas=212141-51-0
BOC Sciences
212142-18-2
http://www.bocsci.com/description.asp?cas=212142-18-2
Capot Chemical
20537
https://www.capotchem.com/search.do?q=20537
Capot Chemical
26251
https://www.capotchem.com/search.do?q=26251
Cayman Chemical
14868
http://www.caymanchem.com/app/template/Product.vm/catalog/14868
Chem Scene
CS-0149
http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0149
ChemShuttle
101091
https://www.chemshuttle.com/catalogsearch/result/?q=101091
ChemShuttle
109833
https://www.chemshuttle.com/catalogsearch/result/?q=109833
Combi-Blocks
QI-6490
http://www.combi-blocks.com/cgi-bin/find.cgi?QI-6490
Combi-Blocks
QJ-3967
http://www.combi-blocks.com/cgi-bin/find.cgi?QJ-3967
Debye Scientific
DB-066452
https://www.debyesci.com/index.php?id=product&ext[cno]=DB-066452
eMolecules
10510651
https://orderbb.emolecules.com/search/#?query=10510651
eMolecules
275129557
https://orderbb.emolecules.com/search/#?query=275129557
eMolecules
32176466
https://orderbb.emolecules.com/search/#?query=32176466
eMolecules
8781495
https://orderbb.emolecules.com/search/#?query=8781495
eNovation Chemicals
D388251
https://www.enovationchem.com/Products.asp?SEARCHTEXT=D388251&searchbtn.x=0&searchbtn.y=0
Excenen
EX-A1398
http://www.excenen.com/searchresultlist.php?id=EX-A1398
Excenen
EX-A334
http://www.excenen.com/searchresultlist.php?id=EX-A334
Exclusive Chemistry
2362
http://www.exchemistry.com/chem-catalog/product-2362.html
Fluorochem
387719
http://www.fluorochem.co.uk/Products/Product?code=387719
Hairui
HR107196
http://www.hairuichem.com/en/product/search.do?q=HR107196
Hairui
HR115093
http://www.hairuichem.com/en/product/search.do?q=HR115093
Hairui
HR129648
http://www.hairuichem.com/en/product/search.do?q=HR129648
KeyOrganics
AS-17435
http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-17435
KeyOrganics
AS-58428
http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-58428
Lab Network
LN01275198
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01275198
Lab Network
LN01355249
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01355249
Life Chemicals
F9995-0196
https://shop.lifechemicals.com/2/F9995-0196
Life Chemicals
F9995-0197
https://shop.lifechemicals.com/2/F9995-0197
Matrix Scientific
138696
http://www.matrixscientific.com/138696.html
Matrix Scientific
143587
http://www.matrixscientific.com/143587.html
Matrix Scientific
146709
http://www.matrixscientific.com/146709.html
mcule
MCULE-1855542614
https://mcule.com/MCULE-1855542614/
mcule
MCULE-1943062725
https://mcule.com/MCULE-1943062725/
mcule
MCULE-3078477385
https://mcule.com/MCULE-3078477385/
MedChem Express
HY-12018
https://www.medchemexpress.com/search.html?q=HY-12018&ft=&fa=&fp=
Molcore
MC110757
http://www.molcore.com/CatMC110757.html
Molnova
M13374
https://www.molnova.com/en/serch-list.html?keywords=M13374
Molnova
M13375
https://www.molnova.com/en/serch-list.html?keywords=M13375
MolPort
MolPort-003-850-836
https://www.molport.com/shop/molecule-link/MolPort-003-850-836
MolPort
MolPort-005-940-840
https://www.molport.com/shop/molecule-link/MolPort-005-940-840
MolPort
MolPort-009-679-410
https://www.molport.com/shop/molecule-link/MolPort-009-679-410
MuseChem
I002633
https://www.musechem.com/product/I002633.html
MuseChem
I011272
https://www.musechem.com/product/I011272.html
MuseChem
R012061
https://www.musechem.com/product/R012061.html
PI Chemicals
PI-37151
http://www.pipharm.com/catalog_products/PI-37151.html
ShangHai Biochempartner
BCP16436
http://www.biochempartner.com/search_BCP16436
ShangHai Biochempartner
BCP24024
http://www.biochempartner.com/search_BCP24024
ShangHai Biochempartner
BCP27632
http://www.biochempartner.com/search_BCP27632
TargetMol
T6720
https://www.targetmol.com/search?keyword=T6720
Tetrahedron
TS39968
http://www.thsci.com/search.do?q=TS39968
Tocris
5680
https://www.tocris.com/search.php?Type=QuickSearch&Value=5680
Toronto Research Chemicals
A780110
https://www.trc-canada.com/product-detail/?CatNum=A780110
Toronto Research Chemicals
V099500
https://www.trc-canada.com/product-detail/?CatNum=V099500
Toronto Research Chemicals
V995035
https://www.trc-canada.com/product-detail/?CatNum=V995035
Vesino Industrial Co Ltd
VA11933
http://www.vsnchem.com/search.do?a=s&psize=20&q=VA11933
W&J PharmaChem
50C1109982
http://wjpharmachem.com/new/searcht.php?keyword=50C1109982
Wonderchem
WD05LI5
http://www.wonder-chem.com/search.html?text=WD05LI5
PubMed

PubMed

TitleDatePubMed
Biological therapy update in colorectal cancer.
2007-04
A phase IB, open-label dose-escalating study of the oral angiogenesis inhibitor PTK787/ZK 222584 (PTK/ZK), in combination with FOLFOX4 chemotherapy in patients with advanced colorectal cancer.
2007-04
Vatalanib: the clinical development of a tyrosine kinase inhibitor of angiogenesis in solid tumours.
2007-03
Small molecule tyrosine kinase inhibitors in the treatment of solid tumors: an update of recent developments.
2007-02
Targeted therapy of breast cancer.
2007
Treatment of metastatic colorectal cancer: from cytotoxic agents to molecular agents and multitargeted strategies.
2006-12
4-(Azolylphenyl)-phthalazin-1-amines: Novel inhibitors of VEGF receptors I and II.
2006-12
Role of platelet-derived growth factor and vascular endothelial growth factor in obliterative airway disease.
2006-11-15
1-(Azolyl)-4-(aryl)-phthalazines: novel potent inhibitors of VEGF receptors I and II.
2006-11
Rational design of RGD-albumin conjugates for targeted delivery of the VEGF-R kinase inhibitor PTK787 to angiogenic endothelium.
2006-11
Metabolism and disposition of vatalanib (PTK787/ZK-222584) in cancer patients.
2006-11
Correlation of relative permeability and relative cerebral blood volume in high-grade cerebral neoplasms.
2006-10
High doses of tyrosine kinase inhibitor PTK787 enhance the efficacy of ischemic hypoxia for the treatment of hepatocellular carcinoma: dual effects on cancer cell and angiogenesis.
2006-09
New molecular targeted therapies in thyroid cancer.
2006-09
Tyrosine kinase inhibitors of vascular endothelial growth factor receptors in clinical trials: current status and future directions.
2006-08-02
Chronic stress promotes tumor growth and angiogenesis in a mouse model of ovarian carcinoma.
2006-08
Biological agents versus chemotherapy in the treatment of colorectal cancer.
2006-07
Ionizing radiation antagonizes tumor hypoxia induced by antiangiogenic treatment.
2006-06-01
Phase 1 study of PTK787/ZK 222584, a small molecule tyrosine kinase receptor inhibitor, for the treatment of acute myeloid leukemia and myelodysplastic syndrome.
2006-06
Biomarkers for assessment of pharmacologic activity for a vascular endothelial growth factor (VEGF) receptor inhibitor, PTK787/ZK 222584 (PTK/ZK): translation of biological activity in a mouse melanoma metastasis model to phase I studies in patients with advanced colorectal cancer with liver metastases.
2006-06
A simple, reproducible method for monitoring the treatment of tumours using dynamic contrast-enhanced MR imaging.
2006-05-22
Growth inhibition of orthotopic anaplastic thyroid carcinoma xenografts in nude mice by PTK787/ZK222584 and CPT-11.
2006-05
[Molecular targets in colon cancer].
2006-04
Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.
2006-03-01
Antagonism of sphingosine-1-phosphate receptors by FTY720 inhibits angiogenesis and tumor vascularization.
2006-01-01
Lessons from phase III clinical trials on anti-VEGF therapy for cancer.
2006-01
Vascular endothelial growth factor receptor signaling is required for cardiac valve formation in zebrafish.
2006-01
Clinical implications of angiogenesis in cancers.
2006
[Some new findings in the pathogenesis of myeloproliferative disorders and new insight into more effective treatment].
2006
Vascular endothelial growth factor contributes to prostate cancer-mediated osteoblastic activity.
2005-12-01
Antivascular therapy of oral tongue squamous cell carcinoma with PTK787.
2005-12
Targeted Therapies in Cancer - Fourth International Congress. Angiogenesis inhibition.
2005-12
Perspectives in colorectal cancer - Sixth Annual Conference. Metastatic colorectal cancer.
2005-12
Update on angiogenesis inhibitors.
2005-11
Anticancer Drug Discovery and Development - SRI's Seventh Annual Summit.
2005-10
Targeting multiple signal transduction pathways in lung cancer.
2005-09
Targeting angiogenesis with vascular endothelial growth factor receptor small-molecule inhibitors: novel agents with potential in lung cancer.
2005-09
PTK787/ZK222584, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor, reduces uptake of the contrast agent GdDOTA by murine orthotopic B16/BL6 melanoma tumours and inhibits their growth in vivo.
2005-08
Phase I study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of PTK787/ZK 222584 administered twice daily in patients with advanced cancer.
2005-06-20
The antitumor and antiangiogenic activity of vascular endothelial growth factor receptor inhibition is potentiated by ErbB1 blockade.
2005-06-15
Enhanced susceptibility of irradiated tumor vessels to vascular endothelial growth factor receptor tyrosine kinase inhibition.
2005-06-15
Phase I clinical and pharmacokinetic study of PTK/ZK, a multiple VEGF receptor inhibitor, in patients with liver metastases from solid tumours.
2005-06
The realisation of targeted antitumour therapy.
2005-06
Angiogenesis and lung cancer: prognostic and therapeutic implications.
2005-05-10
The assessment of antiangiogenic and antivascular therapies in early-stage clinical trials using magnetic resonance imaging: issues and recommendations.
2005-05-09
Vatalanib (PTK787/ZK 222584) in combination with FOLFOX4 versus FOLFOX4 alone as first-line treatment for colorectal cancer: preliminary results from the CONFIRM-1 trial.
2005-05
Phacilitate Cell and Gene Therapy Forum 2005. Cell and gene therapy: a corporate perspective. 24-26 January 2005, Washington, DC, USA.
2005-03
Arterial spin labeling blood flow magnetic resonance imaging for the characterization of metastatic renal cell carcinoma(1).
2005-03
PTK 787/ZK 222584, a tyrosine kinase inhibitor of all known VEGF receptors, represses tumor growth with high efficacy.
2005-03
[Problems in the current target therapy of malignancies].
2005
Patents

Patents

06271233
5
06514974
5
US 6258812
3
WO 9835958
3

Sample Use Guides

In Vivo Use Guide
Curator's Comment: Vatalanib 1,250 mg orally daily in combination with FOLFOX-4. https://www.ncbi.nlm.nih.gov/pubmed/21464406
Vatalanib 1250 mg orally was given once daily (cohort 1) or 750-1250 mg once daily in an intra-patient dose escalating schedule (cohort 2) in 28-day cycles.
Route of Administration: Oral
In Vitro Use Guide
PTK787 (1 micro M) also blocks VEGF-induced migration of MM cells across an extracellular matrix.
Substance Class Chemical
Created
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on Mon Mar 31 18:20:42 GMT 2025
Edited
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on Mon Mar 31 18:20:42 GMT 2025
Record UNII
5DX9U76296
Record Status Validated (UNII)
Record Version
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Name Type Language
VATALANIB
INN   MI   USAN   WHO-DD  
USAN   INN  
Official Name English
BAY-86-5127
Preferred Name English
VATALANIB [USAN]
Common Name English
VATALANIB [MI]
Common Name English
Vatalanib [WHO-DD]
Common Name English
NVP-PTK787
Code English
CGP-79787
Code English
vatalanib [INN]
Common Name English
K-222584
Code English
Classification Tree Code System Code
NCI_THESAURUS C1967
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
NCI_THESAURUS C1742
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
Code System Code Type Description
PUBCHEM
151194
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
FDA UNII
5DX9U76296
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
DRUG BANK
DB04879
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
CAS
212141-54-3
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
EPA CompTox
DTXSID2046919
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
MERCK INDEX
m11400
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY Merck Index
MESH
C404768
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
SMS_ID
100000091584
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
NCI_THESAURUS
C1868
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
ChEMBL
CHEMBL101253
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
EVMPD
SUB26999
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
INN
7994
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
WIKIPEDIA
Vatalanib
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
CHEBI
90620
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
USAN
QQ-50
Created by admin on Mon Mar 31 18:20:42 GMT 2025 , Edited by admin on Mon Mar 31 18:20:42 GMT 2025
PRIMARY
Related Record Type Details
Structure of VATALANIB SUCCINATE
SALT/SOLVATE -> PARENT
Structure of VATALANIB
EXCRETED UNCHANGED
FECAL
Structure of VATALANIB
EXCRETED UNCHANGED
URINE
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 1
TARGET -> INHIBITOR
Related Record Type Details
Structure of 1-PHTHALAZINEMETHANOL, 4-((4-CHLORO-3-HYDROXYPHENYL)AMINO)-.ALPHA.-4-PYRIDINYL-
METABOLITE -> PARENT
MINOR
FECAL
Structure of CGP-85903
METABOLITE -> PARENT
TRACE AMOUNT
FECAL; PLASMA
Structure of ZK-264851
METABOLITE -> PARENT
FECAL
Structure of 2-CHLORO-5-((4-(4-PYRIDINYLMETHYL)-1-PHTHALAZINYL)AMINO)PHENOL
METABOLITE -> PARENT
FECAL
Structure of ZK-261557
METABOLITE -> PARENT
PLASMA
Structure of ZK-260120
METABOLITE -> PARENT
URINE
Structure of ZK-261557
METABOLITE -> PARENT
TRACE AMOUNT
FECAL
Structure of ZK-261557
METABOLITE -> PARENT
URINE
Structure of 1-PHTHALAZINEMETHANOL, 4-((4-CHLOROPHENYL)AMINO)-.ALPHA.-4-PYRIDINYL-
METABOLITE -> PARENT
TRACE AMOUNT
FECAL; PLASMA
Structure of 4-((4-((1-OXIDOPYRIDIN-1-IUM-4-YL)METHYL)PHTHALAZIN-1-YL)AMINO)PHENOL
METABOLITE -> PARENT
MINOR
URINE
Structure of 1-PHTHALAZINEMETHANOL, 4-((4-CHLOROPHENYL)AMINO)-.ALPHA.-4-PYRIDINYL-
METABOLITE -> PARENT
MINOR
URINE
Structure of PHENOL, 2-CHLORO-5-((4-(4-PYRIDINYLMETHYL)-1-PHTHALAZINYL)AMINO)-, 1-(HYDROGEN SULFATE)
METABOLITE -> PARENT
TRACE AMOUNT
FECAL
Structure of 4-((4-(4-PYRIDINYLMETHYL)-1-PHTHALAZINYL)AMINO)PHENOL
METABOLITE -> PARENT
FECAL
Structure of CGP-85903
METABOLITE -> PARENT
MINOR
URINE
Structure of 1-((4-CHLOROPHENYL)(4-(4-PYRIDINYLMETHYL)-1-PHTHALAZINYL)AMINO)-1-DEOXY-.BETA.-D-GLUCOPYRANURONIC ACID
METABOLITE -> PARENT
TRACE AMOUNT
PLASMA
Structure of PHENOL, 2-CHLORO-5-((4-(4-PYRIDINYLMETHYL)-1-PHTHALAZINYL)AMINO)-, 1-(HYDROGEN SULFATE)
METABOLITE -> PARENT
MINOR
URINE
Structure of ZK-260120
METABOLITE -> PARENT
PLASMA
Structure of PHENOL, 2-CHLORO-5-((4-(4-PYRIDINYLMETHYL)-1-PHTHALAZINYL)AMINO)-, 1-(HYDROGEN SULFATE)
METABOLITE -> PARENT
TRACE AMOUNT
FECAL
Structure of ZK-276224
METABOLITE -> PARENT
FECAL
Structure of .BETA.-D-GLUCOPYRANURONIC ACID, 1-((4-CHLOROPHENYL)(4-(4-PYRIDINYLCARBONYL)-1-PHTHALAZINYL)AMINO)-1-DEOXY-
METABOLITE -> PARENT
URINE
Related Record Type Details
Structure of VATALANIB
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC SINGLE ORAL DOSE ADMINISTRATION

AT STEADY-STATE

Biological Half-life PHARMACOKINETIC SINGLE ORAL DOSE ADMINISTRATION

AT STEADY-STATE

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