Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C29H28N6O2.ClH |
| Molecular Weight | 529.033 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CN1CCC(COC2=CN=C(N=C2)C3=CC(CN4N=C(C=CC4=O)C5=CC(=CC=C5)C#N)=CC=C3)CC1
InChI
InChIKey=YHHHGHDGBUUWIS-UHFFFAOYSA-N
InChI=1S/C29H28N6O2.ClH/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;1H
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/25736998
https://www.ncbi.nlm.nih.gov/pubmed/23553846
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/25736998
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.
Originator
Approval Year
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.
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1103508-80-0
Created by
admin on Sat Dec 16 17:16:50 GMT 2023 , Edited by admin on Sat Dec 16 17:16:50 GMT 2023
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NON-SPECIFIC STOICHIOMETRY | |||
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300000044480
Created by
admin on Sat Dec 16 17:16:50 GMT 2023 , Edited by admin on Sat Dec 16 17:16:50 GMT 2023
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PRIMARY | |||
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8B73AZL5XP
Created by
admin on Sat Dec 16 17:16:50 GMT 2023 , Edited by admin on Sat Dec 16 17:16:50 GMT 2023
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25171647
Created by
admin on Sat Dec 16 17:16:50 GMT 2023 , Edited by admin on Sat Dec 16 17:16:50 GMT 2023
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PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD
