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Details

Stereochemistry ACHIRAL
Molecular Formula C29H28N6O2
Molecular Weight 492.5727
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TEPOTINIB

SMILES

CN1CCC(CC1)COc2cnc(-c3cccc(c3)Cn4c(=O)ccc(-c5cccc(c5)C#N)n4)nc2

InChI

InChIKey=AHYMHWXQRWRBKT-UHFFFAOYSA-N
InChI=1S/C29H28N6O2/c1-34-12-10-21(11-13-34)20-37-26-17-31-29(32-18-26)25-7-3-5-23(15-25)19-35-28(36)9-8-27(33-35)24-6-2-4-22(14-24)16-30/h2-9,14-15,17-18,21H,10-13,19-20H2,1H3

HIDE SMILES / InChI

Description
Curator's Comment:: https://www.ncbi.nlm.nih.gov/pubmed/23553846

Tepotinib is an investigational small molecule inhibitor of the c-Met receptor tyrosine kinase. Alterations of the c-Met signaling pathway are found in various cancer types and correlate with aggressive tumor behavior and poor clinical prognosis. Tepotinib is a potent and selective c-Met inhibitor, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib is currently in Phase I/II trials in liver cancer and lung cancer.

Approval Year

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary

Sample Use Guides

500 mg of tepotinib tablet once daily orally during each 21 day cycle
Route of Administration: Oral
Tepotinib inhibits HGF-induced c-Met phosphorylation in A549 cells with IC50 of 6 nM. Treatment with Tepotinib induces a marked reduction of c-Met–constitutive phosphorylation in EBC-1 cells with IC50 of 9 nM. Tepotinib effectively blocks phosphorylation of the major downstream effectors of the c-Met enzyme, such as Grb2, Gab1, Sos, PLCγ, and phosphoinositide 3-kinase, in EBC-1, MKN-45, and Hs746T cells in the range of 1 to 10 nM.
Name Type Language
TEPOTINIB
INN   WHO-DD  
INN   USAN  
Official Name English
MSC-2156119
Code English
TEPOTINIB [WHO-DD]
Common Name English
TEPOTINIB [INN]
Common Name English
MSC2156119
Code English
EMD-1214063
Code English
EMD1214063
Code English
TEPOTINIB [USAN]
Common Name English
MSC-2156119J
Code English
BENZONITRILE, 3-(1,6-DIHYDRO-1-((3-(5-((1-METHYL-4-PIPERIDINYL)METHOXY)-2-PYRIMIDINYL)PHENYL)METHYL)-6-OXO-3-PYRIDAZINYL)-
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C1967
Created by admin on Sat Jun 26 16:28:57 UTC 2021 , Edited by admin on Sat Jun 26 16:28:57 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 16:28:57 UTC 2021 , Edited by admin on Sat Jun 26 16:28:57 UTC 2021
Code System Code Type Description
PUBCHEM
25171648
Created by admin on Sat Jun 26 16:28:57 UTC 2021 , Edited by admin on Sat Jun 26 16:28:57 UTC 2021
PRIMARY
EPA CompTox
1100598-32-0
Created by admin on Sat Jun 26 16:28:57 UTC 2021 , Edited by admin on Sat Jun 26 16:28:57 UTC 2021
PRIMARY
DRUG BANK
DB15133
Created by admin on Sat Jun 26 16:28:57 UTC 2021 , Edited by admin on Sat Jun 26 16:28:57 UTC 2021
PRIMARY
CAS
1100598-32-0
Created by admin on Sat Jun 26 16:28:57 UTC 2021 , Edited by admin on Sat Jun 26 16:28:57 UTC 2021
PRIMARY
INN
9934
Created by admin on Sat Jun 26 16:28:57 UTC 2021 , Edited by admin on Sat Jun 26 16:28:57 UTC 2021
PRIMARY
ChEMBL
CHEMBL3402762
Created by admin on Sat Jun 26 16:28:57 UTC 2021 , Edited by admin on Sat Jun 26 16:28:57 UTC 2021
PRIMARY
FDA UNII
1IJV77EI07
Created by admin on Sat Jun 26 16:28:57 UTC 2021 , Edited by admin on Sat Jun 26 16:28:57 UTC 2021
PRIMARY
NCI_THESAURUS
C88314
Created by admin on Sat Jun 26 16:28:57 UTC 2021 , Edited by admin on Sat Jun 26 16:28:57 UTC 2021
PRIMARY