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Chemical Structure| 790299-79-5 Chemical Structure| 790299-79-5

Structure of Masitinib
CAS No.: 790299-79-5

Chemical Structure| 790299-79-5

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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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Product Details of Masitinib

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

Safety of Masitinib

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

Related Pathways of Masitinib

RTK
cytoskeleton

Isoform Comparison

Biological Activity

Target
  • PDGFRβ

    PDGFRβ, IC50:800 nM

  • PDGFRα

    PDGFRα, IC50:540 nM

  • c-Kit

    Kit, IC50:200 nM

In Vitro:

Cell Line
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:

Species
Animal Model
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 <<

Protocol

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

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

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