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Details

Stereochemistry ACHIRAL
Molecular Formula C20H16ClN5O3
Molecular Weight 409.826
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TELATINIB

SMILES

CNC(=O)C1=NC=CC(COC2=NN=C(NC3=CC=C(Cl)C=C3)C4=C2OC=C4)=C1

InChI

InChIKey=QFCXANHHBCGMAS-UHFFFAOYSA-N
InChI=1S/C20H16ClN5O3/c1-22-19(27)16-10-12(6-8-23-16)11-29-20-17-15(7-9-28-17)18(25-26-20)24-14-4-2-13(21)3-5-14/h2-10H,11H2,1H3,(H,22,27)(H,24,25)

HIDE SMILES / InChI

Molecular Formula C20H16ClN5O3
Molecular Weight 409.826
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Telatinib (Bay-579352) developed by Bayer is an orally available and highly potent inhibitor of tyrosine kinases VEGFR2,VEGFR3, PDGFR and c-Kit. Telatinib is a potent inhibitor of angiogenesis. Telatinib caused a significant decrease in endothelium-dependent and endothelium-independent vasodilation. Telatinib demonstrates anti-tumor activity in various cancer models. Telatinib is ready for phase III clinical trials for the treatment of gastric cancer. In 2010, it has been granted orphan drug status by the FDA. Most frequent adverse events were pain, nausea, voice changes and fatigue.

Originator

Curator's Comment: # Bayer

Approval Year

Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Gateways to clinical trials.
2007 Jan-Feb
Patents

Sample Use Guides

twice-daily continuously, 450-900 mg
Route of Administration: Oral
Telatinib inhibits VEGF-dependent proliferation of human umbilical vein endothelial cells (HUVECs) with an IC50 of 26 nM and PDGF-stimulated growth of human aortic smooth muscle cells with an IC50 of 249 nM.
Substance Class Chemical
Created
by admin
on Sat Dec 16 17:53:02 GMT 2023
Edited
by admin
on Sat Dec 16 17:53:02 GMT 2023
Record UNII
18P7197Q7J
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TELATINIB
INN   WHO-DD  
INN  
Official Name English
4-(((4-((4-CHLOROPHENYL)AMINO)FURO(2,3-D)PYRIDAZIN-7-YL)OXY)METHYL)-N-METHYLPYRIDINE-2-CARBOXAMIDE
Systematic Name English
Telatinib [WHO-DD]
Common Name English
telatinib [INN]
Common Name English
BAY 57-9352
Code English
BAY-579352
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 307410
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
NCI_THESAURUS C1967
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
Code System Code Type Description
EVMPD
SUB32825
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
PRIMARY
NCI_THESAURUS
C80869
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
PRIMARY
SMS_ID
100000126084
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
PRIMARY
PUBCHEM
9808844
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
PRIMARY
INN
8795
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
PRIMARY
FDA UNII
18P7197Q7J
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
PRIMARY
DRUG BANK
DB15393
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
PRIMARY
ChEMBL
CHEMBL2079588
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
PRIMARY
EPA CompTox
DTXSID70954809
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
PRIMARY
CAS
332012-40-5
Created by admin on Sat Dec 16 17:53:02 GMT 2023 , Edited by admin on Sat Dec 16 17:53:02 GMT 2023
PRIMARY
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