TELATINIB

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 Search

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22571661 | https://www.ncbi.nlm.nih.gov/pubmed/18519779 | https://www.ncbi.nlm.nih.gov/pubmed/21378200

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

Approval Year

Targets

Primary Target	Pharmacology	Potency
Vascular endothelial growth factor receptor 2 104 Target ID: CHEMBL279 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22571661 \| https://www.ncbi.nlm.nih.gov/pubmed/18519779	Inhibitor 8297	6.0 nM [IC50]
Vascular endothelial growth factor receptor 3 41 Target ID: CHEMBL1955 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22571661 \| https://www.ncbi.nlm.nih.gov/pubmed/18519779	Inhibitor 8297	4.0 nM [IC50]
Platelet-derived growth factor receptor alpha 30 Target ID: P26618 Gene ID: 18595.0 Gene Symbol: Pdgfra Target Organism: Mus musculus (Mouse) Sources: https://www.ncbi.nlm.nih.gov/pubmed/22571661 \| https://www.ncbi.nlm.nih.gov/pubmed/18519779	Inhibitor 8297	15.0 nM [IC50]
Stem cell growth factor receptor 53 Target ID: CHEMBL1936 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22571661 \| https://www.ncbi.nlm.nih.gov/pubmed/18519779	Inhibitor 8297	1.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Gastric cancer 53 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28052652 http://www.news-medical.net/news/20110228/ACT-Biotech-files-SPA-with-FDA-for-telatinib-combination-Phase-3-trial-for-stomach-cancer.aspx	Primary		Phase III 656	Unknown Approved Use Unknown
Solid tumors 145 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19002179	Primary		Phase I 428	Unknown Approved Use Unknown

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY105440	https://www.001chemical.com/chem/search?q=DY105440
1PlusChem LLC	1P00C70M	https://www.1pchem.com/search?query=1P00C70M
AK Scientific	X7508	https://aksci.com/item_detail.php?cat=X7508
ApexBio Technology	A8550	https://www.apexbt.com/catalogsearch/result/?q=A8550
AstaTech	42291	http://astatechinc.com/CPSResult.php?CRNO=42291
BLD Pharm	BD152516	http://www.bldpharm.com/search/Search.html?keyword=BD152516
Capot Chemical	22596	https://www.capotchem.com/search.do?q=22596
Chem Scene	CS-3722	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-3722
ChemShuttle	101248	https://www.chemshuttle.com/catalogsearch/result/?q=101248
Excenen	EX-A007	http://www.excenen.com/searchresultlist.php?id=EX-A007
Hairui	HR144656	http://www.hairuichem.com/en/product/search.do?q=HR144656
Matrix Scientific	125102	http://www.matrixscientific.com/125102.html
MedChem Express	HY-10527	https://www.medchemexpress.com/search.html?q=HY-10527&ft=&fa=&fp=
MolPort	MolPort-016-633-360	https://www.molport.com/shop/molecule-link/MolPort-016-633-360
Molcore	MC105440	http://www.molcore.com/CatMC105440.html
Molnova	M14115	https://www.molnova.com/en/serch-list.html?keywords=M14115
MuseChem	I003199	https://www.musechem.com/product/I003199.html
Selleck Chemicals	S2231	http://www.selleckchem.com/search.html?searchDTO.searchParam=S2231
ShangHai Biochempartner	BCP000350	http://www.biochempartner.com/search_BCP000350
ShangHai Biochempartner	BCP02409	http://www.biochempartner.com/search_BCP02409
Synthonix	13822	https://synthonix.com/catalogsearch/result/?q=13822
TargetMol	T6166	https://www.targetmol.com/search?keyword=T6166
Toronto Research Chemicals	T015700	https://www.trc-canada.com/product-detail/?CatNum=T015700
eMolecules	36516863	https://orderbb.emolecules.com/search/#?query=36516863
eMolecules	85163657	https://orderbb.emolecules.com/search/#?query=85163657
eNovation Chemicals	D210767	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D210767&searchbtn.x=0&searchbtn.y=0
mcule	MCULE-2706634959	https://mcule.com/MCULE-2706634959/
mcule	MCULE-6157972879	https://mcule.com/MCULE-6157972879/

PubMed

Title	Date	PubMed
Gateways to clinical trials.	2007 Jan-Feb	17344945
Gateways to clinical trials.	2007 Jun	17805439
Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor.	2008 Jun 1	18519779
Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours.	2008 Nov 18	19002179
Gateways to clinical trials.	2008 Oct	19088949
Initial assessment, surveillance, and management of blood pressure in patients receiving vascular endothelial growth factor signaling pathway inhibitors.	2010 May 5	20351338
Gateways to clinical trials.	2010 Sep	21069103

Patents

Sample Use Guides

In Vivo Use Guide

twice-daily continuously, 450-900 mg

Route of Administration: Oral

In Vitro Use Guide

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.

Name

Type

Language

TELATINIB

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