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Chemical Structure| 1029712-80-8 Chemical Structure| 1029712-80-8

Structure of Capmatinib
CAS No.: 1029712-80-8

Chemical Structure| 1029712-80-8

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INCB28060 is a potent and selective c-MET kinase inhibitor. INCB28060 inhibits c-MET kinase activity with an average IC50 of 0.13 nM.

Synonyms: INCB28060; INC280; NVP-INC280

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Product Citations

Product Citations

Wang, Qing ; Li, Mengge ; Gan, Yu ; Jiang, Shuheng ; Qiao, Jie ; Zhang, Wei , et al.

Abstract: Purpose: Pancreatic ductal adenocarcinoma (PDAC) is a malignant disease with a poor prognosis. One prominent aspect of PDAC that contributes to its aggressive behavior is its altered cellular metabolism. The aim of this study was to characterize the oncogenic effects of ubiquinol-cytochrome c reductase core protein I (UQCRC1), a key component of mitochondrial complex III, in PDAC development and to assess its potential as a therapeutic target for PDAC. Experimental Design: The expression of UQCRC1 in human PDAC tissues and p48-Cre/p53Flox/WT/LSL-KrasG12D (KPC) mouse pancreatic intraepithelial neoplasias (PanINs) was determined by immunohistochemistry. The role of UQCRC1 in promoting PDAC growth was evaluated in vitro in PANC-1 and CFPAC-1 cells and in vivo in transplanted mouse models of PDAC. Extracellular flux and RNA-Seq analyses were applied to investigate the mechanism of UQCRC1 in the regulation of mitochondrial metabolism and PDAC cell growth. The therapeutic potential of UQCRC1 in PDAC was assessed by knockdown of UQCRC1 using an RNA interference approach. Results: UQCRC1 expression showed a gradual increase during the progression from PanIN stages to PDAC in KPC mice. Elevated expression of UQCRC1 was observed in 72.3% of PDAC cases and was correlated with poor prognosis of the disease. UQCRC1 promoted PDAC cell growth in both in vitro experiments and in vivo subcutaneous and orthotopic mouse models. UQCRC1 overexpression resulted in increased mitochondrial oxidative phosphorylation (OXPHOS) and ATP production. The overproduced ATP was released into the extracellular space via the pannexin 1 channel and then functioned as an autocrine or paracrine agent to promote cell proliferation through the ATP/P2Y2-RTK/AKT axis. UQCRC1 knockdown or ATP release blockage could effectively inhibit PDAC growth. Conclusion: UQCRC1 has a protumor function and may serve as a potential prognostic marker and therapeutic target for PDAC.

Keywords: Pancreatic Ductal Adenocarcinoma ; UQCRC1 ; Mitochondrial Oxidative Phosphorylation ; Extracellular ATP

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Product Details of Capmatinib

CAS No. :1029712-80-8
Formula : C23H17FN6O
M.W : 412.42
SMILES Code : O=C(NC)C1=CC=C(C2=NN3C(N=C2)=NC=C3CC4=CC=C5N=CC=CC5=C4)C=C1F
Synonyms :
INCB28060; INC280; NVP-INC280
MDL No. :MFCD18633285
InChI Key :LIOLIMKSCNQPLV-UHFFFAOYSA-N
Pubchem ID :25145656

Safety of Capmatinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Capmatinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
WT and Tpl2−/−keratinocytes 0.1 nM 2 h Capmatinib inhibited the HGF-stimulated p-MET and fully blocked the HGF-mediated increase in p-EGFR, restoring levels to baseline conditions. Oncogenesis. 2019 Jan 10;8(1):1.
NF1-MET and NF1-P53 cells 100 nM 72 h To evaluate the sensitivity of NF1-MET and NF1-P53 cells to Capmatinib, the results showed that NF1-P53 cells were resistant to Capmatinib and Trametinib as single agents and in combination therapy. Oncogene. 2024 May;43(19):1411-1430.
PC3M cells 10 nM 24 h To evaluate the effect of Capmatinib on the migration and invasion capacity of PC3M cells. Results showed that Capmatinib significantly reduced the migratory capacity of cells. Mol Oncol. 2025 Feb;19(2):474-495.
PC3 cells 10 nM 24 h To evaluate the effect of Capmatinib on the migration and invasion capacity of PC3 cells. Results showed that Capmatinib significantly reduced the migratory capacity of cells. Mol Oncol. 2025 Feb;19(2):474-495.
EBC-1 1.5, 2.2, 2.4 μM 2 months To establish capmatinib-resistant NSCLC cell lines and evaluate their resistance mechanisms. Results showed that capmatinib-resistant NSCLC cells were dependent on alternative pathway activation. Cancer Res Treat. 2019 Jul;51(3):951-962.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/C nude mice Orthotopic metastatic model Oral 10 mg/kg Once daily for 8 weeks To evaluate the inhibitory effect of Capmatinib combined with Defactinib on ETV1-induced HCC metastasis. J Exp Clin Cancer Res. 2022 Sep 16;41(1):275
Mice Tpl2−/−mice Dietary administration 44 mg/kg Continued for 52 weeks Capmatinib treatment significantly reduced the overall tumor burden in Tpl2?/?mice and prevented all malignant conversion of benign papillomas to invasive SCC. Oncogenesis. 2019 Jan 10;8(1):1.
Mice MPNST xenograft model Oral 30 mg/kg Twice daily for 15 days To evaluate the impact of p53 loss on Capmatinib sensitivity, the results showed that Capmatinib significantly inhibited tumor growth in both NF1-MET and NF1-MET;sgP53 models, but only NF1-MET tumors regressed during treatment, while NF1-MET;sgP53 tumors remained stable, with a subset of tumors showing increased growth. Oncogene. 2024 May;43(19):1411-1430.
Mice NSG-hHGFki mice Oral 10 mg/kg 5 days a week for 4 weeks To evaluate the effect of Capmatinib on tumour growth in NSG-hHGFki mice. Results showed that Capmatinib significantly reduced the tumour volume induced by ETV1 and ERG overexpressing cells. Mol Oncol. 2025 Feb;19(2):474-495.
Mice Hepa1-6, HCA-1 and DEN HCC models Oral 10 mg/kg Once daily for 5 days The combination of Capmatinib with PD-1 blockade significantly enhanced antitumor efficacy in HCC models, particularly in the αPD-1 refractory DEN model, outperforming the type II inhibitor Cabozantinib. J Immunother Cancer. 2024 Oct 30;12(10):e009690

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03693339 Cancer|Lung Cancer Metastatic|... More >>MET Gene Mutation Less << PHASE2 UNKNOWN 2022-06-30 Asan Medical Center, Seoul, 05... More >>505, Korea, Republic of Less <<
NCT05567055 Non-small Cell Lung Cancer PHASE2 WITHDRAWN 2025-09-28 -
NCT02019693 Kidney Cancer PHASE2 COMPLETED 2021-12-17 National Institutes of Health ... More >>Clinical Center, 9000 Rockville Pike, Bethesda, Maryland, 20892, United States Less <<
NCT02414139 Carcinoma, Non-Small-Cell Lung PHASE2 COMPLETED 2023-05-16 Pacific Shores Medical Group S... More >>C, Long Beach, California, 90813, United States|University Of California Los Angeles Dept of Onc, Los Angeles, California, 90095, United States|University of California Irvine Medical Center Chao Family Chao Family Comp Cancer Center, Orange, California, 92868, United States|H Lee Moffitt Cancer Center and Research Institute ., Tampa, Florida, 33612, United States|University of Iowa Hospitals and Clinics SC-3, Iowa City, Iowa, 52242, United States|Massachusetts General Hospital MGH Cancer Center, Boston, Massachusetts, 02114, United States|VA Ann Arbor Health System VA Ann Arbor Health System, Ann Arbor, Michigan, 48105, United States|Mayo Clinic Rochester ., Rochester, Minnesota, 55905, United States|Oregon Health and Science University SC, Portland, Oregon, 97239, United States|Lehigh Valley Health Network SC, Allentown, Pennsylvania, 18103, United States|Andrew and Patel Associates, Camp Hill, Pennsylvania, 17011, United States|Mays Cancer Ctr Uthsa Mdacc SC-5, San Antonio, Texas, 78229, United States|University of Utah / Huntsman Cancer Institute Oncology, Salt Lake City, Utah, 84103, United States|Novartis Investigative Site, Caba, Buenos Aires, C1426ANZ, Argentina|Novartis Investigative Site, Buenos Aires, Caba, C1431FWO, Argentina|Novartis Investigative Site, La Rioja, 5300, Argentina|Novartis Investigative Site, Wien, 1210, Austria|Novartis Investigative Site, Leuven, 3000, Belgium|Novartis Investigative Site, Marseille cedex 20, Bouches Du Rhone, 13915, France|Novartis Investigative Site, Dijon, Cote D Or, 21034, France|Novartis Investigative Site, Clermont-Ferrand, 63011, France|Novartis Investigative Site, La Tronche, 38700, France|Novartis Investigative Site, Lille, 59000, France|Novartis Investigative Site, Marseille, 13273, France|Novartis Investigative Site, Paris, 75970, France|Novartis Investigative Site, Pierre Benite, 69495, France|Novartis Investigative Site, Rennes, 35043, France|Novartis Investigative Site, Strasbourg Cedex, 67091, France|Novartis Investigative Site, Heidelberg, Baden-Württemberg, 69126, Germany|Novartis Investigative Site, Berlin, 13125, Germany|Novartis Investigative Site, Frankfurt, 60590, Germany|Novartis Investigative Site, Gottingen, 37075, Germany|Novartis Investigative Site, Halle (Saale), 06120, Germany|Novartis Investigative Site, Hamburg, 20251, Germany|Novartis Investigative Site, Hannover, 30625, Germany|Novartis Investigative Site, Homburg, 66421, Germany|Novartis Investigative Site, Koeln, 50937, Germany|Novartis Investigative Site, Muenchen, 81925, Germany|Novartis Investigative Site, Nuernberg, 90419, Germany|Novartis Investigative Site, Ravensburg, 88214, Germany|Novartis Investigative Site, Tuebingen, 72076, Germany|Novartis Investigative Site, Ulm, 89081, Germany|Novartis Investigative Site, Ramat Gan, 52621, Israel|Novartis Investigative Site, Tel Aviv, 6423906, Israel|Novartis Investigative Site, Bologna, BO, 40138, Italy|Novartis Investigative Site, Brescia, BS, 25123, Italy|Novartis Investigative Site, Catania, CT, 95124, Italy|Novartis Investigative Site, Catanzaro, CZ, 88100, Italy|Novartis Investigative Site, Meldola, FC, 47014, Italy|Novartis Investigative Site, Firenze, FI, 50134, Italy|Novartis Investigative Site, Monza, MB, 20900, Italy|Novartis Investigative Site, Milano, MI, 20141, Italy|Novartis Investigative Site, Milano, MI, 20162, Italy|Novartis Investigative Site, Modena, MO, 41124, Italy|Novartis Investigative Site, Roma, RM, 00155, Italy|Novartis Investigative Site, Verona, VR, 37126, Italy|Novartis Investigative Site, Napoli, 80131, Italy|Novartis Investigative Site, Nagoya, Aichi, 464 8681, Japan|Novartis Investigative Site, Nagoya, Aichi, 466 8560, Japan|Novartis Investigative Site, Fukuoka-city, Fukuoka, 811-1395, Japan|Novartis Investigative Site, Akashi, Hyogo, 673-8558, Japan|Novartis Investigative Site, Sendai city, Miyagi, 980 0873, Japan|Novartis Investigative Site, Okayama-city, Okayama, 700-8558, Japan|Novartis Investigative Site, Osaka Sayama, Osaka, 589 8511, Japan|Novartis Investigative Site, Chuo ku, Tokyo, 104 0045, Japan|Novartis Investigative Site, Koto ku, Tokyo, 135 8550, Japan|Novartis Investigative Site, Ube-city, Yamaguchi, 755-0241, Japan|Novartis Investigative Site, Bundang Gu, Gyeonggi Do, 13620, Korea, Republic of|Novartis Investigative Site, Gyeonggi do, Korea, 10408, Korea, Republic of|Novartis Investigative Site, Seoul, 03080, Korea, Republic of|Novartis Investigative Site, Ashrafieh, 166830, Lebanon|Novartis Investigative Site, Mexico, Distrito Federal, 14080, Mexico|Novartis Investigative Site, Amsterdam, 1066 CX, Netherlands|Novartis Investigative Site, Groningen, 9713 GZ, Netherlands|Novartis Investigative Site, Maastricht, 6229 HX, Netherlands|Novartis Investigative Site, Rotterdam, 3015 GD, Netherlands|Novartis Investigative Site, Oslo, NO 0424, Norway|Novartis Investigative Site, Moscow, 109028, Russian Federation|Novartis Investigative Site, Saint Petersburg, 192148, Russian Federation|Novartis Investigative Site, Tambov, 392000, Russian Federation|Novartis Investigative Site, Singapore, 119228, Singapore|Novartis Investigative Site, Singapore, 168583, Singapore|Novartis Investigative Site, Sevilla, Andalucia, 41009, Spain|Novartis Investigative Site, Oviedo, Asturias, 33011, Spain|Novartis Investigative Site, Barcelona, Catalunya, 08035, Spain|Novartis Investigative Site, Barcelona, Catalunya, 08036, Spain|Novartis Investigative Site, La Coruna, Galicia, 15006, Spain|Novartis Investigative Site, Madrid, 28034, Spain|Novartis Investigative Site, Madrid, 28041, Spain|Novartis Investigative Site, Stockholm, SE-171 76, Sweden|Novartis Investigative Site, Kaohsiung, 82445, Taiwan|Novartis Investigative Site, Taipei, 10002, Taiwan|Novartis Investigative Site, Taoyuan, 33305, Taiwan|Novartis Investigative Site, Birmingham, B9 5SS, United Kingdom|Novartis Investigative Site, London, W6 8RF, United Kingdom Less <<
NCT02474537 Hepatic Impairment PHASE1 COMPLETED 2017-09-12 University of Miami Miller Sch... More >>ool of Medicine Clinical Resea Oncology, Miami, Florida, 33136, United States|Clinical Pharmacology of Miami, LLC., Miami, Florida, 33142, United States|Orlando Clinical Research Center, Orlando, Florida, 32086, United States|DaVita Clinical Research, Minneapolis, Minnesota, 55404, United States|Duke University Medical Center Oncology, Durham, North Carolina, 27710, United States Less <<
NCT01546428 Advanced Solid Tumor PHASE1 COMPLETED 2025-01-16 Novartis Investigative Site, K... More >>ashiwa, Chiba, 277-8577, Japan|Novartis Investigative Site, Fukuoka, 811-1395, Japan Less <<
NCT05154344 MET Alterations|Non Small Cell... More >> Lung Cancer|METex14 Mutations Less << COMPLETED 2022-02-01 CHU, Lille, France|CHU, Tours,... More >> France Less <<
NCT01737827 Advanced Hepatocellular Carcin... More >>oma With c-MET Dysregulation Less << PHASE2 TERMINATED 2023-05-24 Novartis Investigative Site, N... More >>anjing, Jiangsu, 210002, China|Novartis Investigative Site, Xi'an, Shanxi, 710032, China|Novartis Investigative Site, Hangzhou, Zhejiang, 310016, China|Novartis Investigative Site, Hong Kong, Hong Kong|Novartis Investigative Site, Singapore, 168583, Singapore|Novartis Investigative Site, Khon Kaen, THA, 40002, Thailand|Novartis Investigative Site, Bangkok, 10330, Thailand|Novartis Investigative Site, Bangkok, 10700, Thailand Less <<
NCT05675683 Metastatic Non-Small Cell Lung... More >> Cancer Less << COMPLETED 2021-12-31 18 Novartis Investigative Site... More >>s in the US, East Hanover, New Jersey, 07936-1080, United States Less <<
NCT03240393 Carcinoma|Non-Small-Cell Lung ... More >>Cancer Less << PHASE2 WITHDRAWN 2021-10-26 -
NCT02925104 cMET Dysegulation Advanced Sol... More >>id Tumors Less << PHASE1 COMPLETED 2018-05-16 Indiana University Simon Cance... More >>r Center SC, Indianapolis, Indiana, 46202, United States|Novartis Investigative Site, Salzburg, 5020, Austria|Novartis Investigative Site, Herlev, 2730, Denmark|Novartis Investigative Site, Dresden, 01307, Germany|Novartis Investigative Site, Mainz, 55131, Germany|Novartis Investigative Site, Nijmegen, 6500 HB, Netherlands|Novartis Investigative Site, Malaga, Andalucia, 29010, Spain|Novartis Investigative Site, Santiago de Compostela, Galicia, 15706, Spain|Novartis Investigative Site, Barcelona, 08041, Spain|Novartis Investigative Site, Madrid, 28040, Spain|Novartis Investigative Site, Zaragoza, 50009, Spain|Novartis Investigative Site, Goteborg, 413 45, Sweden|Novartis Investigative Site, Lund, SE-221 85, Sweden|Novartis Investigative Site, Stockholm, 171 76, Sweden|Novartis Investigative Site, Uppsala, SE-751 85, Sweden|Novartis Investigative Site, London, W1G 6AD, United Kingdom|Novartis Investigative Site, Manchester, M20 4BX, United Kingdom Less <<
NCT04741789 Carcinoma, Non-Small Cell Lung... More >>|Non-Small Cell Lung Cancer|Non-Small-Cell Lung Carcinoma|Nonsmall Cell Lung Cancer Less << AVAILABLE - -
NCT01324479 Solid Tumors PHASE1 COMPLETED 2017-07-04 Highlands Oncology Group, Faye... More >>tteville, Arkansas, 72703, United States|University of Chicago SC, Chicago, Illinois, 60637, United States|Karmanos Cancer Institute Wayne St Karmanos, Detroit, Michigan, 48201, United States|Sarah Cannon Research Institute Dept of Onc, Nashville, Tennessee, 37203, United States|University of Texas/MD Anderson Cancer Center Dept of Onc, Houston, Texas, 77030-4009, United States|Novartis Investigative Site, Westmead, New South Wales, 2145, Australia|Novartis Investigative Site, Woolloongabba, Queensland, 4102, Australia|Novartis Investigative Site, Ottawa, Ontario, K1H 8L6, Canada|Novartis Investigative Site, Toronto, Ontario, M5G 2M9, Canada|Novartis Investigative Site, La Tronche, 38700, France|Novartis Investigative Site, LILLE Cédex, 59037, France|Novartis Investigative Site, Strasbourg Cedex, 67091, France|Novartis Investigative Site, Essen, 45147, Germany|Novartis Investigative Site, Frankfurt, 60590, Germany|Novartis Investigative Site, Freiburg, 79106, Germany|Novartis Investigative Site, Gottingen, 37075, Germany|Novartis Investigative Site, Hannover, 30625, Germany|Novartis Investigative Site, Oldenburg, 26121, Germany|Novartis Investigative Site, Hong Kong, Hong Kong|Novartis Investigative Site, Shatin, New Territories, Hong Kong|Novartis Investigative Site, Haifa, 3525408, Israel|Novartis Investigative Site, Kfar Saba, 4428164, Israel|Novartis Investigative Site, Ramat Gan, 5265601, Israel|Novartis Investigative Site, Tel Aviv, 6423906, Israel|Novartis Investigative Site, Ancona, AN, 60126, Italy|Novartis Investigative Site, Meldola, FC, 47014, Italy|Novartis Investigative Site, Milano, MI, 20133, Italy|Novartis Investigative Site, Milano, MI, 20162, Italy|Novartis Investigative Site, Reggio Emilia, RE, 42123, Italy|Novartis Investigative Site, Seoul, Gyeonggi Do, 03080, Korea, Republic of|Novartis Investigative Site, Gyeonggi do, Korea, 10408, Korea, Republic of|Novartis Investigative Site, Seoul, Korea, 05505, Korea, Republic of|Novartis Investigative Site, Seoul, Korea, 06351, Korea, Republic of|Novartis Investigative Site, Seoul, Seocho Gu, 06591, Korea, Republic of|Novartis Investigative Site, Utrecht, The Netherlands, 3508 GA, Netherlands|Novartis Investigative Site, Amsterdam, 1066 CX, Netherlands|Novartis Investigative Site, Rotterdam, 3075 EA, Netherlands|Novartis Investigative Site, Oslo, NO-0424, Norway|Novartis Investigative Site, Singapore, 169610, Singapore|Novartis Investigative Site, Granada, Andalucia, 18014, Spain|Novartis Investigative Site, Oviedo, Asturias, 33006, Spain|Novartis Investigative Site, Barcelona, Catalunya, 08035, Spain|Novartis Investigative Site, Madrid, 28046, Spain|Novartis Investigative Site, Zaragoza, 50009, Spain|Novartis Investigative Site, Tainan, Taiwan ROC, 70403, Taiwan|Novartis Investigative Site, Taipei, Taiwan ROC, 10041, Taiwan|Novartis Investigative Site, Songkhla, Hat Yai, 90110, Thailand Less <<
NCT04460729 Non-small Cell Lung Carcinoma ... More >>(NSCLC) Less << PHASE2 WITHDRAWN 2023-11-17 -
NCT04677595 Non-Small Cell Lung Cancer (NS... More >>CLC) Less << PHASE2 ACTIVE_NOT_RECRUITING 2025-12-31 Novartis Investigative Site, X... More >>iamen, Fujian, 361001, China|Novartis Investigative Site, Foshan, Guangdong, 528000, China|Novartis Investigative Site, Guang Zhou, Guangdong, 510120, China|Novartis Investigative Site, Guangzhou, Guangdong, 510080, China|Novartis Investigative Site, Guangzhou, Guangdong, 510515, China|Novartis Investigative Site, Harbin, Heilongjiang, 150081, China|Novartis Investigative Site, Zhengzhou, Henan, 450003, China|Novartis Investigative Site, Wuhan, Hubei, 430022, China|Novartis Investigative Site, Shenyang, Liaoning, 110011, China|Novartis Investigative Site, Jinan, Shandong, 250117, China|Novartis Investigative Site, Shanghai, Shanghai, 200032, China|Novartis Investigative Site, Shanghai, Shanghai, 200433, China|Novartis Investigative Site, Chengdu, Sichuan, 610041, China|Novartis Investigative Site, Kunming, Yunnan, 650106, China|Novartis Investigative Site, Hangzhou, Zhejiang, 310022, China|Novartis Investigative Site, Beijing, 100036, China|Novartis Investigative Site, Tianjin, 300052, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.12mL

2.42mL

1.21mL

24.25mL

4.85mL

2.42mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. 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
 

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