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Home > Encyclopedia > Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl]

Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl]

Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl] structure

Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl] 

structure
  • CAS No:

    1100598-32-0

  • Formula:

    C29H28N6O2

  • Chemical Name:

    Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl]

  • Synonyms:

    Veledimex;3-(1-(3-(5-((1-Methylpiperidin-4-yl)methoxy)pyrimidin-2-yl)benzyl)-6-oxo-1,6-dihydropyridazin-;Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl];3-(1-(3-(5-((1-Methylpiperidin-4-yl)Methoxy)pyriMidin-2-yl)benzyl)-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile;EMD-1214063;3-[1,6-Dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]benzonitrile;Tepotinib;Tepotinib (EMD 1214063)

  • Categories:

    Biochemical Engineering  >  Inhibitors

Description

EMD 1214063 is a potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. IC50 Value: 4 nM [1]Target: c-Metin vitro: EMD 1214063 inhibits HGF-induced c-Met phosphorylation in A549 cells with IC50 of 6 nM. Treatment with EMD 1214063 induces a marked reduction of c-Met–constitutive phosphorylation in EBC-1 cells with IC50 of 9 nM. EMD 1214063 effectively blocka phosphorylation of the major downstream effectors of the c-Met


Tepotinib is under investigation in clinical trial NCT03531762 (Effect of a Proton Pump Inhibitor on the Pharmacokinetics (PK) of Tepotinib).|Tepotinib is a Kinase Inhibitor. The mechanism of action of tepotinib is as a Mesenchymal Epithelial Transition Inhibitor, and P-Glycoprotein Inhibitor.|Tepotinib is an orally bioavailable inhibitor of MET tyrosine kinase with potential antineoplastic activity. Tepotinib selectively binds to MET tyrosine kinase and disrupts MET signal transduction pathways, which may induce apoptosis in tumor cells overexpressing this kinase. The receptor tyrosine kinase MET (also known as hepatocyte growth factor receptor or HGFR), is the product of the proto-oncogene c-Met and is overexpressed or mutated in many tumor cell types; this protein plays key roles in tumor cell proliferation, survival, invasion, and metastasis, and tumor angiogenesis.

Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl] Basic Attributes

492.57162

492.227386

1IJV77EI07

DTXSID70149132

C88314

L - Antineoplastic and immunomodulating agents

Characteristics

94.7

3.4

1.25

626.5±65.0 °C(Predicted)

332.7±34.3 °C

1.660

Drug Information

Treatment of non-small cell lung carcinoma (NSCLC)|Drug: Tepotinibhydrochloride

Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)

3-(1-(3-(5-((1-Methyl-4-piperidinyl)methoxy)-2-pyrimidinyl)benzyl)-6-oxo-1,6-dihydro-3-pyridazinyl)benzonitrile

Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl] Use and Manufacturing

Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:492.6
XLogP3:3.4
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:7
Exact Mass:492.22737416
Monoisotopic Mass:492.22737416
Topological Polar Surface Area:94.7
Heavy Atom Count:37
Complexity:880
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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