Tepotinib

Binding Mode

Product Name: Tepotinib
CAS No.: 1100598-32-0
Chemical Name: Tepotinib
Synonyms: Tepotinib;EMD-1214063;Veledimex;CS-977;MSC2156119;EMD1214063,Tepotinib;epotinib(EMD 1214063);EMD 1214063; EMD1214063;Tepotinib (EMD 1214063);EMD-1214063|||MSC2156119
CBNumber: CB72550731
Molecular Formula: C29H28N6O2
Formula Weight: 492.57
MOL File: 1100598-32-0.mol

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Tepotinib Property

Boiling point:: 626.5±65.0 °C(Predicted)
Density: 1.25
storage temp.: Store at -20°C
form: Solid
pka: 8.93±0.10(Predicted)
Water Solubility: ≥ 4.93 mg/mL in DMSO, <2.52 mg/mL in EtOH, <2.56 mg/mL in Water
InChI: 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
InChIKey: AHYMHWXQRWRBKT-UHFFFAOYSA-N
SMILES: C(#N)C1=CC=CC(C2=NN(CC3=CC=CC(C4=NC=C(OCC5CCN(C)CC5)C=N4)=C3)C(=O)C=C2)=C1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 18492
Product name: EMD 1214063
Purity: ≥98%
Packaging: 1mg
Price: $35
Updated: 2021/12/16

Cayman Chemical

Product number: 18492
Product name: EMD 1214063
Purity: ≥98%
Packaging: 5mg
Price: $123
Updated: 2021/12/16

Cayman Chemical

Product number: 18492
Product name: EMD 1214063
Purity: ≥98%
Packaging: 10mg
Price: $228
Updated: 2021/12/16

Cayman Chemical

Product number: 18492
Product name: EMD 1214063
Purity: ≥98%
Packaging: 25mg
Price: $481
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb181238
Product name: Tepotinib(EMD-1214063)
Purity: >98%
Packaging: 100mg
Price: $690.2
Updated: 2021/12/16

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Tepotinib Chemical Properties,Usage,Production

Binding Mode

In the co-crystal structure of tepotinib bound to MET (Fig. 1), the pyrimidine nitrogen hydrogen bonds with the amide NH group of Met1160 (the third hinge residue) and the pyridazinone oxygen hydrogen bonds to the amide NH group of DFG-Asp1222 (Fig. 2). The inhibitor binds to a DFG-in and αC-out inactive conformation as a type I½ inhibitor.

Description

Tepotinib is a highly selective inhibitor against MET. In xenograft models, acquired resistance to EGFR TKIs via secondary EGFR T790 M mutations can be overcome with tepotinib treatment.

Uses

EMD 1214063 is a novel ATP-comptetitive inhibitor of the MET hepatocyte growth factor receptor and a novel kinase inhibitor and a therapeutic agent for neuroblastoma. Potent c-MET inhibitor.

brand name

Tepmetko

General Description

Class: receptor tyrosine kinase; Treatment: NSCLC with METex14; Other name: EMD-1214063; Oral bioavailability = 72%; Elimination half-life = 32 h; Protein binding = 94%

Mechanism of action

Tepotinib is a Kinase Inhibitor. The mechanism of action of tepotinib is as a Mesenchymal Epithelial Transition Inhibitor, and P-Glycoprotein Inhibitor.

Pharmacology

Tepotinib is a highly-selective inhibitor of MET kinase activity, with an average IC50 of approximately 1.7 nmol/L. It has a moderate duration of action necessitating once-daily administration. Tepotinib has been associated with the development of interstitial lung disease (ILD)/pneumonitis, which can sometimes be fatal. Patients should be monitored closely for signs of new or worsening respiratory symptoms (e.g. dyspnea, cough), and treatment with tepotinib should be immediately withheld if ILD/pneumonitis is suspected. If no other potential causes of ILD/pneumonitis are identified, therapy with tepotinib should be suspended indefinitely.

Clinical Use

Tepotinib is currently being evaluated in combination with EGFR TKI gefitinib and also a separate trial in NSCLC patients with MET exon 14 skipping mutation and MET amplification.

Side effects

anxiety
chest pain or tightness
difficult or labored breathing
dizziness or lightheadedness
fast heartbeat
fever or chills
general feeling of discomfort or illness
muscle or bone pain

Synthesis

The synthesis of Tepotinib is as follows:
Acetonitrile (700 ml) was added to the reaction vessel, and the compound represented by formula 7a (37.63 g, 0.1 mol), the compound represented by formula 8 (23.66 g, 0.12 mol), and potassium carbonate (34.55 g, 0.25 mol) were added under stirring.and tetrabutylammonium bromide (1.93g, 0.006mol), the reaction system was stirred and heated to reflux, and the reaction was stirred at reflux for 12h. After the reaction was completed, the temperature was cooled to room temperature, the reaction solution was concentrated under reduced pressure to dryness, and ethanol (360ml) was added. ), stir to dissolve, slowly add 1.5 mol/l hydrochloric acid aqueous solution dropwise, adjust the pH value to 1-2, cool down to 5-7 °C, stir and crystallize for 6 h, filter, and vacuum dry the solid at 45 °C for 6 h to obtain formula 1. The compound (44.42 g) was shown in a yield of 81.2% and a purity of 99.7% by HPLC.

target

Primary target: MET

Drug interactions

Tepotinib is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) who have mesenchymal-epithelial transition (_MET_) exon 14 skipping alterations.

Metabolism

Tepotinib is metabolized primarily by CYP3A4 and CYP2C8, with some apparent contribution by unspecified UGT enzymes. The metabolite M506 is the major circulating metabolite, comprising approximately 40.4% of observed drug material in plasma, while the M668 glucuronide metabolite has been observed in plasma at much lower quantities (~4% of an orally administered dose). A total of 10 phase I and phase II metabolites have been detected following tepotinib administration, most of which are excreted in the feces.

Tepotinib Preparation Products And Raw materials

Raw materials

Preparation Products

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Tepotinib Suppliers

China 143 India 3 United States 17 Global 163

MedChemexpress LLC

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AdooQ BioScience, LLC

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Target molecule Corp.

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Musechem

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TargetMol Chemicals Inc.

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InvivoChem

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Cckinase, Inc.

Tel: +1 (732)236-3202
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Country: United States
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BOC Sciences

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Creative Enzymes

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Cayman Chemical Company

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Matrix Scientific

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Selleck Chemicals LLC

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View Lastest Price from Tepotinib manufacturers

Nanjing Fred Technology Co., Ltd

Product: Tepotinib 1100598-32-0
Price: US $0.00-0.00/kg
Min. Order: 1kg
Purity: 99%, Single impurity＜0.1
Supply Ability: 1 ton
Release date: 2023-12-20

Shanghai CRM New Material Technology Co., LTD

Product: tepotinib 1100598-32-0
Price: US $10.00-15.00/g
Min. Order: 10g
Purity: 99%
Supply Ability: 10t
Release date: 2022-09-22

Career Henan Chemical Co

Product: Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl] 1100598-32-0
Price: US $1.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 20kg
Release date: 2019-12-23

1100598-32-0, TepotinibRelated Search:

H-MET-SER-ARG-PRO-ALA-CYS-PRO-ASN-ASP-LYS-TYR-GLU-OH Titanium 2,3,6-TRICHLOROBENZOIC ACID delta-Hexalactone Ceritinib MK-2206 2HCl PD 0325901 Trametinib Ibrutinib Crizotinib

CS-977

EMD 1214063; EMD1214063

3-[1-[[3-[5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl]phenyl]methyl]-6-oxopyridazin-3-yl]benzonitrile

epotinib(EMD 1214063)

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-(3-(5-((1-METHYLPIPERIDIN-4-YL)METHOXY)PYRIMIDIN-2-YL)BENZYL)-1,6-DIHYDRO-6-OXOPYRIDAZIN-3-YL)B

3-[1,6-Dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]benzonitrile

EMD1214063,Tepotinib

Tepotinib

Tepotinib (EMD 1214063)

MSC2156119

3-[1,6-Dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]benzonitrile EMD-1214063

EMD-1214063 3-[1,6-Dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]benzonitrile

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] USP/EP/BP

Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)

EMD-1214063|||MSC2156119

1100598-32-0

100598-32-0

110050.98-32-0

Inhibitors

API