Structure of Masitinib
CAS No.: 790299-79-5
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Masitinib is an inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms.
Synonyms: AB1010; Masican; Masiviera
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
CAS No. : | 790299-79-5 |
Formula : | C28H30N6OS |
M.W : | 498.64 |
SMILES Code : | O=C(NC1=CC=C(C(NC2=NC(C3=CC=CN=C3)=CS2)=C1)C)C4=CC=C(CN5CCN(CC5)C)C=C4 |
Synonyms : |
AB1010; Masican; Masiviera
|
MDL No. : | MFCD09954132 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
Target |
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In Vitro:
Concentration | Treated Time | Description | References |
A549 cells | 10 µM | 2 days | inhibition of SARS-CoV-2 infection | PMC8809056 |
293T cells | 10 µM | inhibition of 3CL protease activity | PMC8809056 | |
CCRF-CEM cells | 10 µM | 72 hours | Evaluate the anti-proliferative effect of Masitinib in the T-ALL cell line CCRF-CEM, results showed that Masitinib was unable to inhibit cancer cell proliferation. | PMC10227015 |
HUVEC | 0.3, 1, 3 µM | 12 hours | To evaluate the inhibitory effect of Masitinib on HUVEC cell migration, results showed that Masitinib significantly inhibited VEGF-induced HUVEC cell migration. | PMC10657461 |
HCAEC | 0.3, 1, 3 µM | 12 hours | To evaluate the inhibitory effect of Masitinib on HCAEC cell migration, results showed that Masitinib significantly inhibited VEGF-induced HCAEC cell migration. | PMC10657461 |
NI-1 cells | 0.1 – 0.2 µM | 48 h | To evaluate the inhibitory effect of Masitinib on the proliferation of NI-1 cells, the results showed that Masitinib had a weak inhibitory effect on the proliferation of NI-1 cells. | PMC3401908 |
C2 cells | 0.025 – 0.05 µM | 48 h | To evaluate the inhibitory effect of Masitinib on the proliferation of C2 cells, the results showed that Masitinib had a good inhibitory effect on the proliferation of C2 cells. | PMC3401908 |
HMC-1.1 cells | 0.005 – 0.01 µM | 48 h | To evaluate the inhibitory effect of Masitinib on the proliferation of HMC-1.1 cells, the results showed that Masitinib had a good inhibitory effect on the proliferation of HMC-1.1 cells. | PMC3401908 |
HMC-1.2 cells | >2 µM | 48 h | To evaluate the inhibitory effect of Masitinib on the proliferation of HMC-1.2 cells, the results showed that Masitinib had a weak inhibitory effect on the proliferation of HMC-1.2 cells. | PMC3401908 |
In Vivo:
Administration | Dosage | Frequency | Description | References |
mice | K18-hACE2 transgenic mice | oral | 25 mg/kg or 50 mg/kg | Once daily for 14 days | reduction of SARS-CoV-2 viral load, improvement in lung inflammation and survival rate | PMC8809056 |
Mice | NOD-SCID-IL2Rγc null (NSG) mouse model | Intraperitoneal injection | 25 mg/kg | twice daily for 10 days | Evaluate the anti-leukemic effect of OR0642 in combination with dT in a T-ALL mouse model, results showed that the combination therapy significantly reduced leukemic burden and prolonged mouse survival. | PMC10227015 |
Mice | CAWS-induced KD murine model | Oral | 10 μmol/kg | Single injection | To evaluate the regulatory effect of Masitinib on cardiovascular pathology in the KD murine model, results showed that Masitinib significantly reduced VEGF-induced endothelial cell migration and improved vascular and cardiac inflammatory damage. | PMC10657461 |
Mice | SOD1G93A mouse model | Oral gavage | 5% Palmitic Acid | Continued for 20 weeks | Masitinib reduced the number of mast cells and the influx of mast cell precursors in the spinal cord of ALS mice by inhibiting c-Kit, and improved microvascular pathology. | PMC8361844 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT00831922 | Rheumatoid Arthritis | Phase 2 | Completed | - | - |
NCT00831974 | Mastocytosis | Phase 2 | Completed | - | - |
NCT01045577 | Psoriasis | Phase 2 | Completed | - | - |
NCT01433497 | Multiple Sclerosis, Secondary ... More >>Progressive Multiple Sclerosis, Primary Progressive Multiple Sclerosis, Relapse Free Less << | Phase 3 | Active, not recruiting | March 2019 | Spain ... More >> Hospital de la Santa Creu i Sant Pau Barcelona, Spain, 08041 Less << |
NCT01450488 | Multiple Sclerosis | Phase 2 | Completed | - | - |
NCT00842270 | Asthma | Phase 2 | Completed | - | - |
NCT00866138 | Multiple Myeloma | Phase 2 | Completed | - | France ... More >> Hopital Saint Louis Paris, France Less << |
NCT02605044 | Metastatic Colorectal Cancer | Phase 3 | Terminated(Sponsor decision ba... More >>sed on portfolio prioritization) Less << | - | France ... More >> Hopital Europeen George Pomipidou, Hepato-Gastro-enterologie, 20 rue Leblanc Paris, France, 75 Singapore National Cancer Center, 11 Hospital Drive Singapore, Singapore, 169610 United Kingdom Hammersmith Hospital, Department of Cancer Medicine, Imperial College Healthcare Trust, Du Cane Road London, United Kingdom, W12 0HS Less << |
NCT00789633 | Pancreatic Cancer | Phase 3 | Completed | - | - |
NCT02490488 | Ovarian Cancer | Phase 2 Phase 3 | Recruiting | December 2020 | France ... More >> Institut Sainte Catherine Recruiting Avignon, France, 84000 Contact: Julien GRENIER, MD Less << |
NCT00812240 | Gastrointestinal Stromal Tumor... More >>s Less << | Phase 3 | Terminated(Sponsor decision ba... More >>sed on portfolio prioritization) Less << | - | - |
NCT01266369 | Mastocytosis | Phase 2 | Completed | - | - |
NCT01506336 | Gastro Intestinal Stromal Tumo... More >>r Less << | Phase 2 | Completed | - | France ... More >> Institute Gustave Roussy (IGR) Villejuif, France, 94815 Less << |
NCT03127267 | Amyotrophic Lateral Sclerosis | Phase 3 | Not yet recruiting | May 2024 | - |
NCT02009423 | Gastro-Intestinal Stromal Tumo... More >>ur Less << | Phase 3 | Terminated(Sponsor decision ba... More >>sed on portfolio prioritization) Less << | - | - |
NCT01449162 | Asthma | Phase 3 | Active, not recruiting | March 2019 | Hungary ... More >> University of Debrecen Medical and Health Science Center Debrecen, Hungary, 4032 Less << |
NCT01872598 | Alzheimer Disease | Phase 3 | Active, not recruiting | October 2019 | Spain ... More >> Hospital Universitario Ramón y Cajal Madrid, Spain, 28034 Less << |
NCT01694277 | Gastrointestinal Stromal Tumor... More >>s Less << | Phase 3 | Recruiting | December 2022 | France ... More >> Institut Bergonié Recruiting Bordeaux, France, 33000 Less << |
NCT00998751 | Gastro-intestinal Stromal Tumo... More >>urs Less << | Phase 2 | Completed | - | France ... More >> Lecesne Villejuif, France Less << |
NCT01410695 | Rheumatoid Arthritis (RA) | Phase 2 Phase 3 | Terminated(Sponsor decision ba... More >>sed on portfolio prioritization) Less << | - | Czechia ... More >> ARTMEDI UPD s.r.o Hostivice, Czechia, 25301 Less << |
NCT01470131 | Multiple Myeloma | Phase 3 | Terminated(Sponsor decision ba... More >>sed on portfolio prioritization) Less << | - | United States, Illinois ... More >> Medical and Surgical Specialists Galesburg, Illinois, United States, 61401 United States, Maryland Center for Cancer and Blood Disorders Bethesda, Maryland, United States, 20817 United States, North Carolina Carolinas Medical Center Charlotte, North Carolina, United States, 28203 Southeastern Medical Oncology Center Goldsboro, North Carolina, United States, 27534 United States, Wisconsin Froedtert & Medical College of Wisconsin-CLCC Milwaukee, Wisconsin, United States, 53226 France CHU Estaing Clermont Ferrand, France Centre Hospitalier Sud Francilien Corbeil-Essonnes, France CH Le Mans Le Mans, France Hôpital Universitaire Dupuytren Limoges, France Hôpital Ambroise Paré Marseille, France Hôpital de l'Hôtel Dieu Nantes, France Hôpital Saint Louis Paris, France Centre Hospitalier Saint Jean Perpignan, France Less << |
NCT03766295 | Locally Advanced or Metastatic... More >> Pancreatic Cancer Less << | Phase 3 | Recruiting | December 2020 | France ... More >> Centre Hospitalier de Longjumeau Recruiting Longjumeau, France, 91160 Less << |
NCT00976118 | Alzheimer's Disease | Phase 2 | Completed | - | - |
NCT00814073 | Indolent Systemic Mastocytosis | Phase 3 | Completed | - | United States, California ... More >> UC Davis Health System , Department of Dermatology Sacramento, California, United States, 95816 United States, Texas MD Anderson Cancer Centre Houston, Texas, United States, 77030 France CHU d'Amiens Amiens, France Hôpital Avicenne Bobigny, France CHU de Brest Brest, France CHU de Caen Caen, France CHU Clermont Ferrand Clermont Ferrand, France, 63000 Hôpital Claude Huriez Lille, France CHU Dupuytren Limoges, France Hôpital Ambroise Paré Marseille, France Hôpital Nord Marseille, France Hôpital Central Nancy, France CHU Hôtel Dieu Nantes, France Hôpital l'Archet II Nice, France Hôpital Necker Paris, France Hôpital Tenon Paris, France CHU Lyon Sud Pierre Bénite, France, 69495 Centre Hospitalier Lyon Sud Pierre-Bénite, France CHU Milétrie Poitiers, France CHU Hôpital Sud Rennes, France CHU de Saint-Etienne Saint-Etienne, France Hôpital Purpan Toulouse, France Hôpital Bretonneau Tours, France Hôpital des Hauts Clos Troyes, France Less << |
NCT03761225 | Metastatic Castrate Resistant ... More >>Prostate Cancer Less << | Phase 3 | Recruiting | September 2020 | France ... More >> Polyclinique d'oncologie de Gentilly Recruiting Nancy, France, 54100 Contact: Dominique Spaeth, MD Less << |
NCT02588677 | Amyotrophic Lateral Sclerosis ... More >>(ALS) Less << | Phase 2 Phase 3 | Completed | - | Spain ... More >> Hospital Carlos III Madrid, Spain, 28029 Less << |
NCT03556956 | Colorectal Cancer Metastatic | PHASE2|PHASE3 | COMPLETED | 2025-12-20 | University Hospital Olomouc, O... More >>lomouc, 779 00, Czechia|Chu - Hopitaux de Rouen, Rouen, France|Omsk Clinical oncology dispensary, Omsk, 644013, Russian Federation|Hospital Madrid Norte San Chinarro, Madrid, Spain|Hammersmith Hospital Imperial College Healthcare Nhs Trust, London, United Kingdom Less << |
NCT00913432 | Rheumatoid Arthritis | Phase 2 | Completed | - | - |
NCT01280565 | Metastatic Melanoma | Phase 3 | Recruiting | December 2020 | France ... More >> Hôpital Sainte Marguerite Recruiting Marseille, France, 13274 Contact: Jean-Jacques GROB, MD, PhD Less << |
NCT03771040 | Asthma | Phase 3 | Recruiting | December 2020 | Hungary ... More >> University of Debrecen Medical and Health Science Center Recruiting Debrecen, Hungary, 4032 Less << |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.01mL 0.40mL 0.20mL |
10.03mL 2.01mL 1.00mL |
20.05mL 4.01mL 2.01mL |
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Dissolving Methods |
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. 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:
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