Home Cart Sign in  
Chemical Structure| 1100598-32-0 Chemical Structure| 1100598-32-0

Structure of Tepotinib
CAS No.: 1100598-32-0

Chemical Structure| 1100598-32-0

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

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.

Synonyms: EMD 1214063; MSC2156119; EMD-1214063

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of Tepotinib

CAS No. :1100598-32-0
Formula : C29H28N6O2
M.W : 492.57
SMILES Code : N#CC1=CC=CC(C(C=C2)=NN(CC3=CC=CC(C4=NC=C(OCC5CCN(C)CC5)C=N4)=C3)C2=O)=C1
Synonyms :
EMD 1214063; MSC2156119; EMD-1214063
MDL No. :MFCD18452823
InChI Key :AHYMHWXQRWRBKT-UHFFFAOYSA-N
Pubchem ID :25171648

Safety of Tepotinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Tepotinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
EBC-1 5 µM 12 months To generate Tepotinib-resistant cell lines to study resistance mechanisms. PMC7718487
Hs746T 5 µM 12 months To generate Tepotinib-resistant cell lines to study resistance mechanisms. PMC7718487
SNU620 9 nM 48 hours Tepotinib significantly induced apoptosis in SNU620 cells and significantly reduced the protein levels of phosphorylated and total c-MET, phosphorylated and total ERK, β-catenin, and c-MYC. PMC7503648
MKN45 7 nM 48 hours Tepotinib significantly induced apoptosis in MKN45 cells and significantly reduced the protein levels of phosphorylated and total c-MET, phosphorylated and total ERK, β-catenin, and c-MYC. PMC7503648
KATO III 10 nM 48 hours Tepotinib significantly induced apoptosis in KATO III cells but had minimal effects on the protein levels of phosphorylated and total c-MET, phosphorylated and total ERK, β-catenin, and c-MYC. PMC7503648
MHCC97H cells 10 nM 48 hours To evaluate the antiproliferative activity of compound 8b, the results showed an IC50 value of 10 nM against MHCC97H cells. PMC9921947
H358 0-18 µM 72 hours To evaluate the antitumor effects of Tepotinib in combination with Omeprazole, the results showed that the combination significantly reduced cell viability. PMC11167791
A549 0-7.9 µM 72 hours To evaluate the antitumor effects of Tepotinib in combination with Omeprazole, the results showed that the combination significantly reduced cell viability. PMC11167791
NCI-H460/TPT10 cells 1 and 3 μM Tepotinib significantly enhanced the cytotoxicity of ABCG2 substrate drugs mitoxantrone and topotecan, reducing the IC50 values in drug-resistant cells. PMC9136566
HEK293/ABCG2-WT cells 1 and 3 μM Tepotinib significantly enhanced the cytotoxicity of ABCG2 substrate drugs mitoxantrone and topotecan, reducing the IC50 values in drug-resistant cells. PMC9136566
HCCLM3 cells 0.013 µM To evaluate the cytotoxicity of compound 8b against HCCLM3 cells, the results showed an IC50 value of 0.013 μM. PMC9921947
LO2 cells 4.314 µM To evaluate the cytotoxicity of compound 8b against LO2 cells, the results showed an IC50 value of 4.314 μM. PMC9921947
97H cells (human liver cancer cells) 0.013 µM (IC50) To evaluate the anti-tumor activity of the compounds, compound 31e showed the best inhibitory effect with an IC50 value of 26 nM PMC6470795
Pc9 cells (human non-small cell lung cancer cells) 8.105 μM (IC50) To evaluate the inhibitory activity of compound 31e against Pc9 cells, the IC50 value was 42.9 μM PMC6470795
Hela cells (human epithelial cervical cancer cells) 11.22 μM (IC50) To evaluate the inhibitory activity of compound 31e against Hela cells, the IC50 value was >50 μM PMC6470795
SJSA1 cells (human osteosarcoma cells) 12.17 μM (IC50) To evaluate the inhibitory activity of compound 31e against SJSA1 cells, the IC50 value was >50 μM PMC6470795
LO2 cells (human normal liver cells) 10.33 μM (IC50) To evaluate the inhibitory activity of compound 31e against LO2 cells, the IC50 value was >50 μM PMC6470795
HLF cells (human embryonic lung fibroblast cells) 9.44 μM (IC50) To evaluate the inhibitory activity of compound 31e against HLF cells, the IC50 value was >50 μM PMC6470795

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice NCI-H460/TPT10 tumor xenograft model Subcutaneous injection 30 mg/kg Every 3 days until the end of the experiment Tepotinib significantly enhanced the antitumor effect of topotecan in drug-resistant tumors, increasing intratumoral drug accumulation. PMC9136566
Nu/Nu mice H358 cell-derived tumor xenograft model Subcutaneous injection 5 mg/kg Once daily for three weeks To evaluate the in vivo antitumor effects of Tepotinib in combination with Omeprazole, the results showed that the combination significantly inhibited tumor growth. PMC11167791
Rat Sprague‒Dawley rats Oral 50 mg/kg Single dose To study the drug-drug interaction between Tepotinib and naringenin, the results showed that naringenin significantly increased the plasma exposure of Tepotinib and decreased its clearance rate. PMC11536652
Nude mice MKN45 xenograft model Oral 10 mg/kg Once daily for 3 weeks Tepotinib significantly inhibited tumor growth and increased ECAD expression while decreasing phosphorylated c-MET protein levels. PMC7503648
Mice EBC-1 xenograft model Oral 5 mg/kg Once daily, continuous treatment To evaluate the inhibitory effect of Tepotinib in combination with SHP2 inhibitor on tumor growth. PMC7718487
Mice NSCLC xenograft models Oral gavage 100 mg/kg Daily for 32 days To evaluate the antitumor effects of Tepotinib in combination with various EGFR TKIs in NSCLC xenograft models. The results showed that Tepotinib combined with EGFR TKIs effectively inhibited tumor growth, especially in models with high c-Met expression, where Tepotinib alone or in combination exhibited significant antitumor activity. PMC5411803

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04647838 Solid Tumor|MET Exon 14 Skippi... More >>ng Mutation|MET Amplification Less << PHASE2 UNKNOWN 2024-08-31 Chonnam National University Hw... More >>asun Hospital, Hwasun, Chonnam, Korea, Republic of|Chungbuk National University Hospital, Cheongju-si, Chungcheongbuk-do, 28644, Korea, Republic of|Dankook University Hospital, Cheonan, Korea, Republic of|Keimyung University Dongsan Hospital, Daegu, Korea, Republic of|Konyang University Hospital, Daejeon, Korea, Republic of|National Cancer Center, Goyang-si, Korea, Republic of|Hallym University Dongtan Sacred Heart Hospital, Hwaseong-si, Korea, Republic of|Gachon University Gil Medical Center, Incheon, Korea, Republic of|The Catholic University of Korea Incheon St. Marry Hospital, Incheon, Korea, Republic of|Gyeongsang National University Hospital, Jinju, Korea, Republic of|Inje University Haeundae Pain Hospital, Pusan, Korea, Republic of|Kosin University Gaspel Hospital, Pusan, Korea, Republic of|Seoul National University Bundang Hospital, Seongnam-si, Korea, Republic of|Chungang University Hospital, Seoul, Korea, Republic of|Gangnam Severance Hospital, Seoul, Korea, Republic of|Inje University Sanggye Paik Hospital, Seoul, Korea, Republic of|Korea University Anam Hospital, Seoul, Korea, Republic of|Korea University Guro Hospital, Seoul, Korea, Republic of|Samsung Medical Center, Seoul, Korea, Republic of|Seoul National University Hospital, Seoul, Korea, Republic of|Severance Hospital, Seoul, Korea, Republic of|Pusan National University Yangsan Hospital, Yangsan, Korea, Republic of Less <<
NCT02864992 Advanced (Stage IIIB/IV) Non-s... More >>mall Cell Lung Cancer (NSCLC) With MET Exon 14 (METex14) Skipping Alterations or MET Amplification|Lung Adenocarcinoma Stage IIIB/IV Less << PHASE2 ACTIVE_NOT_RECRUITING 2025-10-31 City of Hope Cancer Center, Du... More >>arte, California, 91010, United States|California Cancer Associates for Research & Excellence, Inc., Encinitas, California, 92024, United States|St. Joseph Hospital, Orange, California, 92868-4225, United States|Torrance Health Association, Redondo Beach, California, 90277, United States|St Joseph Heritage Healthcare, Santa Rosa, California, 95403, United States|Rocky Mountain Cancer Centers, LLP, Denver, Colorado, 80218, United States|Holy Cross Hospital Inc., Fort Lauderdale, Florida, 33308, United States|H. Lee Moffitt Cancer Center and Research Institute, Inc, Tampa, Florida, 33612-9497, United States|University Cancer & Blood Center, LLC, Athens, Georgia, 30607, United States|Winship Cancer Institute, Atlanta, Georgia, 30322, United States|University of Chicago Medical Center, Chicago, Illinois, 60637, United States|Ingalls Hospital, Harvey, Illinois, 60426-3558, United States|Community Regional Cancer Care, Indianapolis, Indiana, 46250, United States|Center for Cancer and Blood Disorders, Bethesda, Maryland, 20817, United States|For Recruiting Locations in the United States, please Contact U.S. Medical Information, Rockland, Massachusetts, United States|St. Louis Cancer Care, LLP, Bridgeton, Missouri, 63044, United States|Saint Louis University Cancer Center, Saint Louis, Missouri, 63110, United States|Saint Louis University, Saint Louis, Missouri, 63110, United States|Summit Medical Group, P.A., Berkeley Heights, New Jersey, 07922, United States|Summit Medical Group, Berkeley Heights, New Jersey, 07922, United States|Regional Cancer Care Associates East Brunswick, East Brunswick, New Jersey, 08816, United States|Somerset Hematology Oncology Associates - Somerville Location, East Brunswick, New Jersey, 8816, United States|Hackensack University Medical Center PARTNER, Hackensack, New Jersey, 07601, United States|Prospect Medical Offices, LLC, Midland Park, New Jersey, 07432, United States|The Valley Hospital, Ridgewood, New Jersey, 07450, United States|Memorial Sloan Kettering Cancer Center - Commack, Commack, New York, 11725, United States|Memorial Sloan Kettering Cancer Center, West Harrison Regional Outpatient Pavilion, Harrison, New York, 10604, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10022, United States|UC Health Clinical Trials Office, Cincinnati, Ohio, 45229, United States|University of Cincinnati - PARENT, Cincinnati, Ohio, 45267-0502, United States|Tennessee Oncology, Nashville, Tennessee, 37203, United States|Vanderbilt University Medical Center, Nashville, Tennessee, 37232, United States|Texas Oncology, P.A. - Austin, Austin, Texas, 78731, United States|Texas Oncology, PA, Beaumont, Texas, 77702-1449, United States|University of Texas MD Anderson Cancer Center, Houston, Texas, 77030, United States|Virginia Cancer Specialists, PC, Fairfax, Virginia, 22031, United States|Swedish Medical Center, Seattle, Washington, 98104, United States|Wenatchee Valley Hospital & Clinics - ATTN: Jay Johnson, Wenatchee, Washington, 98801, United States|Wenatchee Valley Medical Center Oncology, Wenatchee, Washington, 98801, United States|LKH - Universit?tsklinikum der PMU Salzburg - Innere Med III/H?matologie und Onkologie, Salzburg, Austria|UZ Antwerpen, Edegem, 2650, Belgium|UZ Antwerpen, Edegem, Belgium|CHU Ambroise Paré, Mons, 7000, Belgium|CHU Ambroise Paré, Mons, Belgium|AZ Delta, Roeselare, 8800, Belgium|AZ Delta, Roeselare, Belgium|Beijing Hospital, Beijing, China|Peking University Cancer Hospital, Beijing, China|Jilin Cancer Hospital - Oncology, Changchun, China|Hunan Cancer Hospital, Changsha, China|Sichuan Cancer Hospital, Chengdu, China|West China Hospital, Sichuan University, Chengdu, China|Guangdong General Hospital, Guangzhou, China|Zhejiang Cancer Hospita, Hangzhou, China|Affiliated Tumor Hospital of Harbin Medical University, Harbin, China|Anhui Provincial Cancer Hospital aka West Branch of Anhui Province Hospital, Hefei City, China|Jinan Central Hospital, Jinan, China|Linyi Tumor Hospital, Linyi, China|Jiangsu Province Hospital, Nanjing, China|Shanghai Cancer Hospital, Fudan University, Shanghai, China|Liaoning Cancer Hospital & Institute, Shenyang, China|The Affiliated Cancer Hospital of Xinjiang Medical university, Urumqi, China|Groupe Hospitalier Sud - H?pital Haut-Lévêque, Pessac, Gironde, 33604, France|CHU de Toulouse - H?pital Larrey, Toulouse, Haute Garonne, 31059, France|ICO - Site René Gauducheau, Saint Herblain, Loire Atlantique, 44805, France|Clinique Mutualiste de l'Estuaire, Saint Nazaire Cedex, Loire Atlantique, 44606, France|ICO - Site Paul Papin, Angers Cedex 2, Maine Et Loire, 49055, France|Centre Hospitalier de Cholet, Cholet, Maine Et Loire, 49300, France|Centre Hospitalier de Bretagne Sud, Lorient cedex, Morbihan, 56322, France|Hopital Albert Calmette - CHU Lille, Lille Cedex, Nord, 59037, France|Centre Hospitalier de la c?te Basque, Bayonne, Pyrenees Atlantiques, 64100, France|Centre Hospitalier Départemental Les Oudairies, La Roche sur Yon, Vendee, 85925, France|ICO - Site Paul Papin, Angers Cedex 2, France|Centre Hospitalier de la c?te Basque, Bayonne, France|Centre Hospitalier de Cholet, Cholet, France|Centre Hospitalier Intercommunal de Créteil, Creteil cedex, France|Centre Hospitalier Départemental Les Oudairies, La Roche sur Yon, France|Hopital Albert Calmette - CHU Lille, Lille Cedex, France|Centre Hospitalier de Bretagne Sud, Lorient cedex, France|H?pital Saint-Louis, Paris Cedex 10, France|Groupe Hospitalier Sud - H?pital Haut-Lévêque, Pessac, France|ICO - Site René Gauducheau, Saint Herblain, France|Clinique Mutualiste de l'Estuaire, Saint Nazaire Cedex, France|CHU de Toulouse - H?pital Larrey, Toulouse, France|POIS Leipzig GbR, Leipzig, Sachsen, 04357, Germany|Charite Universitaetsmedizin Berlin - Campus Charite Mitte, Berlin, Germany|Klinikum Chemnitz gGmbH, Chemnitz, Germany|For Recruiting Locations outside US, please Contact Merck KGaA Communication Center, Darmstadt, Germany|Staedtisches Klinikum Dresden Standort Dresden-Friedrichstadt, Dresden, Germany|Universitaetsklinikum Carl Gustav Carus TU Dresden, Dresden, Germany|Helios Klinikum Erfurt, Erfurt, Germany|Asklepios Fachkliniken Muenchen-Gauting, Gauting, Germany|SRH Wald-Klinikum Gera gGmbH, Gera, Germany|Universitaetsmedizin Goettingen, Goettingen, Germany|Evangelisches Krankenhaus Hamm GmbH, Hamm, Germany|Universitaetsklinikum Heidelberg, Heidelberg, Germany|Universitaetsklinikum des Saarlandes, Homburg / Saar, Germany|POIS Leipzig GbR, Leipzig, Germany|Universitaetsmedizin der Johannes Gutenberg-Universitaet Mainz, Mainz, Germany|Pius-Hospital Oldenburg, Oldenburg, Germany|Soroka University Medical Center, Beer-Sheva, Israel|Hadassah University Hospital - Ein Kerem, Jerusalem, Israel|Meir Medical Center, Kfar- Saba, Israel|Rabin Medical Center-Beilinson Campus, Petach Tikva, Israel|Tel Aviv Sourasky Medical Center, Tel Aviv, Israel|Istituto Nazionale per la Ricerca sul Cancro di Genova, Genova, Italy|Fondazione IRCCS Istituto Nazionale dei Tumori, Milano, 20133, Italy|Fondazione IRCCS Istituto Nazionale dei Tumori, Milano, Italy|IEO Istituto Europeo di Oncologia, Milano, Italy|Seconda Università degli Studi di Napoli, Napoli, Italy|Azienda Ospedaliera di Padova, Padova, Italy|IOV - Istituto Oncologico Veneto IRCCS, Padova, Italy|Ospedale Santa Maria di Cà Foncello, Padova, Italy|Azienda Ospedaliera San Camillo Forlanini, Roma, Italy|Università Campus Bio-Medico di Roma, Roma, Italy|Istituto Clinico Humanitas, Rozzano, Italy|NHO Kyushu Medical Center, Fukuoka-shi, Japan|National Cancer Center Hospital East, Kashiwa-shi, Japan|Saitama Cancer Center, Kitaadachi-gun, Japan|Kurume University Hospital, Kurume-shi, Japan|NHO Shikoku Cancer Center, Matsuyama-shi, Japan|Nagoya University Hospital, Nagoya-shi, Japan|Niigata Cancer Center Hospital, Niigata-shi, Japan|Osaka International Cancer Institute, Osaka-shi, Japan|NHO Kinki-Chuo Chest Medical Center, Sakai-shi, Japan|Hokkaido University Hospital, Sapporo-shi, Japan|NHO Yamaguchi - Ube Medical Center, Ube-shi, Japan|Kanagawa Cancer Center, Yokohama-shi, Japan|Tottori University Hospital, Yonago-shi, Japan|Dong-A University Hospital, Busan, Korea, Republic of|Kosin University Gospel Hospital, Busan, Korea, Republic of|Kyungpook National University Medical Center, Daegu, Korea, Republic of|National Cancer Center, Goyang-si, Korea, Republic of|Chonnam National University Hwasun Hospital, Hwasun-gun, Korea, Republic of|Gachon University Gil Medical Center, Incheon, Korea, Republic of|Seoul National University Bundang Hospital, Seongnam-si, Korea, Republic of|Korea University Anam Hospital, Seoul, Korea, Republic of|Samsung Medical Center, Seoul, Korea, Republic of|Severance Hospital, Yonsei University, Seoul, Korea, Republic of|The Catholic University of Korea, Seoul St. Mary's Hospital, Seoul, Korea, Republic of|The Catholic University of Korea, St. Vincent's Hospital, Suwon-si, Korea, Republic of|Antoni van Leeuwenhoek Ziekenhuis, Amsterdam, Netherlands|VU Medisch Centrum, Amsterdam, Netherlands|Universitair Medisch Centrum Groningen (UMCG) - Parent, Groningen, Netherlands|Uniwersytecki Szpital Kliniczny w Bialymstoku - Dept of Pulmonology & Tuberculosis, Bialystok, Poland|Centrum Pulmonologii i Torakochirurgii w Bystrej, Bystra, Poland|Dr n med. Slawomir Mandziuk Specjalistyczna Praktyka Lekarska, Lublin, Poland|NZOZ Olsztynski Osr. Onkologiczny "Kopernik" Sp.z o.o, Olsztyn, Poland|Przychodnia Med-Polonia Sp. z o.o., Poznan, 60-693, Poland|Przychodnia Med-Polonia Sp. z o.o., Poznan, Poland|Centrum Onkologii-Instytut im. M. Sklodowskiej Curie, Warszawa, 02-781, Poland|Centrum Onkologii-Instytut im. M. Sklodowskiej Curie, Warszawa, Poland|Hospital Universitari Vall d'Hebron, Barcelona, 08035, Spain|Hospital Universitari Quiron Dexeus, Barcelona, Spain|Hospital Universitari Sagrat Cor, Barcelona, Spain|Hospital Universitari Vall d'Hebron, Barcelona, Spain|Hospital General Universitario Santa Lucia, Cartagena, Spain|Hospital de Especialidades de Jerez de la Frontera - Servicio de Oncologia, Jerez de la Frontera, Spain|Hospital Universitario HM Madrid Sanchinarro, Madrid, 28050, Spain|Hospital General Universitario Gregorio Mara?on, Madrid, Spain|Hospital Universitario 12 de Octubre, Madrid, Spain|Hospital Universitario HM Madrid Sanchinarro, Madrid, Spain|Hospital Universitario La Paz, Madrid, Spain|Hospital Clinico Universitario Virgen de la Victoria, Malaga, Spain|Hospital Universitario Infanta Sofia, San Sebastian de los Reyes, Spain|Hospital General de Catalunya, Sant Cugat del Valles, Spain|Hospital Universitario Virgen Macarena, Sevilla, 41009, Spain|Hospital Universitario Nuestra Se?ora de Valme, Sevilla, Spain|Hospital Universitario Virgen Macarena, Sevilla, Spain|Inselspital - Universitaetsspital Bern - Klinik und Poliklinik für Medizinische Onkologie, Bern, Switzerland|Universitaetsspital Zuerich - Klinik fuer Onkologie, Zuerich, Switzerland|Kaohsiung Chang Gung Memorial Hospital, Kaohsiung, Taiwan|China Medical University Hospital, Taichung, Taiwan|Taichung Veterans General Hospital, Taichung, Taiwan|National Taiwan University Hospital, Taipei, Taiwan|Taipei Veterans General Hospital, Taipei, Taiwan|Tri-Service General Hospital, Taipei, Taiwan Less <<
NCT04739358 Advanced Non-Small Cell Lung C... More >>ancer With MET Mutations Less << PHASE1|PHASE2 TERMINATED 2023-06-23 UC Davis Comprehensive Cancer ... More >>Center, Sacramento, California, 95817, United States|University of Colorado Cancer Center, Aurora, Colorado, 80045, United States|Georgetown Lombardi Comprehensive Cancer Center, Washington, District of Columbia, 20007, United States|UPMC Hillman Cancer Center, Pittsburgh, Pennsylvania, 15232, United States|University of Washington, Seattle, Washington, 98195, United States Less <<
NCT03546608 Hepatic Impairment PHASE1 COMPLETED 2019-02-05 Qps Mra, Llc, Miami, Florida, ... More >>33143, United States|Orlando Clinical Research Center, Orlando, Florida, 32809, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.15mL

2.03mL

1.02mL

20.30mL

4.06mL

2.03mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

Categories