Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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Other Sizes |
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Purity: ≥98%
Masitinib (formerly also known as AB1010) is a novel, potent, orally bioavailable, selective and multi-targeted inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, it shows weak inhibition to ABL and c-Fms. Masitinib selectively binds to and inhibits PDGFR, FGFR3, c-Kit (the stem cell factor receptor), and, to a lesser extent, FAK. It also selectively binds to and mutates the stem cell factor receptor (SCFR). Consequently, in cancer cell types that overexpress these RTKs, tumor cell proliferation may be inhibited.
Targets |
Kit (IC50 = 200 nM); Lyn B (IC50 = 510 nM); PDGFRα (IC50 = 540 nM); PDGFRβ (IC50 = 800 nM); Abl1 (IC50 = 1.20 μM)
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
A 96-well microtitre plate is coated with 0.25 mg/mL poly(Glu, Tyr 4:1) for an entire night. It is then rinsed twice with 250 µL of washing buffer (10 mM phosphate-buffered saline [pH 7.4] and 0.05% Tween 20) and allowed to dry at room temperature for two hours. The assays are conducted at room temperature in a final volume of 50 µL of kinase buffer (10 mM MgCl2, 1 mM MnCl2, 1 mM sodium orthovanadate, 20 mM HEPES, pH 7.8) that contains recombinant enzyme and ATP at a concentration of at least twice the Km for each enzyme to guarantee a linear reaction rate. The enzyme is added to start the reaction, and it is stopped by adding one reaction volume (50 μL) of 100 mM EDTA per 5mol/Lurea mix. Plates are triple-washed and then incubated with tetramethylbenzidine and a 1:30,000 horseradish peroxidase-conjugated anti-phosphotyrosine monoclonal antibody. Spectrophotometry is used to measure the final reaction product at 450 nm.
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Cell Assay |
Microtitre plates are seeded with 104 cells/well in 100 μL of RPMI 1640 medium containing 10% foetal bovine serum at 37°C in order to conduct the Ba/F3 cell proliferation assay. 250 ng/mL of murine SCF or 0.1% of conditioned medium from X63-IL-3 cells are added to these, or not. Purified from the conditioned medium of SCF-producing CHO cells is the murine SCF that activates Kit. Masitinib-grown cells are incubated for 48 hours at 37°C with WST-1 reagent (10 μL/well) for three hours. Using a scanning multiwell spectrophotometer, the absorbance at 450 nm of the formazan dye indicates how much of it has formed. The spectrophotometer's background control is a blank well devoid of cells.
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Animal Protocol |
At 7 weeks old, male Nog-SCID mice are housed in a pathogen-free environment with filtered water and food available at all times. They experience a 12-hour light/12-hour dark cycle. According to the above description, Mia Paca-2 cells are cultured. Mice are given an injection into the right flank at day 0 (D0) containing 107 Mia Paca-2 cells in 200 µL PBS. After a tumor reaches the target size of approximately 200 mm3, it is allowed to grow for 1.5 to 4 weeks. In order to ensure that the mean body weight and tumor volume of each treatment group are well matched, animals are divided into four groups by day 28 (n = 7–8). The animals receive treatment for a maximum of four weeks, following which they are sacrificed. The treatments were as follows: a) daily gavage with 100 mg/kg masitinib; b) intraperitoneal (i.p.) injection of 50 mg/kg gemcitabine twice a week; c) daily gavage with 100 mg/kg masitinib; or d) a combination of daily gavage with 100 mg/kg masitinib and i.p. injection of 50 mg/kg gemcitabine twice a week. Callipers are used to measure the size of tumors, and the formula volume=(length × width2)/2 is used to estimate the tumor volume. (100) × (median tumor volume of treated group)/(median tumor volume of control group) is the formula for the tumor growth inhibition ratio.
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References |
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Molecular Formula |
C28H30N6OS
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Molecular Weight |
498.64
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Exact Mass |
498.22
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Elemental Analysis |
C, 67.44; H, 6.06; N, 16.85; O, 3.21; S, 6.43
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CAS # |
790299-79-5
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Related CAS # |
Masitinib mesylate;1048007-93-7
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Appearance |
Off-white to pale yellow solid powder
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SMILES |
CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC(=CS4)C5=CN=CC=C5
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InChi Key |
WJEOLQLKVOPQFV-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C28H30N6OS/c1-20-5-10-24(16-25(20)31-28-32-26(19-36-28)23-4-3-11-29-17-23)30-27(35)22-8-6-21(7-9-22)18-34-14-12-33(2)13-15-34/h3-11,16-17,19H,12-15,18H2,1-2H3,(H,30,35)(H,31,32)
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Chemical Name |
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-yl-1,3-thiazol-2-yl)amino]phenyl]benzamide
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Synonyms |
AB-1010; AB 1010; AB1010; Masitinib; Brand name: Kinavet; Masivet.
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 4% DMSO+30% PEG 300+5% Tween 80+ddH2O: 30mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0055 mL | 10.0273 mL | 20.0545 mL | |
5 mM | 0.4011 mL | 2.0055 mL | 4.0109 mL | |
10 mM | 0.2005 mL | 1.0027 mL | 2.0055 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05441488 | Recruiting | Drug: Placebo Drug: Masitinib (4.5) |
Progressive Multiple Sclerosis | AB Science | June 28, 2022 | Phase 3 |
NCT05047783 | Recruiting | Drug: Masitinib Mesylate Drug: Placebo |
Covid19 SARS-CoV2 Infection |
AB Science | November 23, 2021 | Phase 2 |
NCT05564169 | Not yet recruiting | Drug: Placebo Drug: Masitinib (4.5) |
Alzheimer Disease | AB Science | January 2024 | Phase 3 |
NCT04333108 | Recruiting | Drug: Masitinib Other: Placebo |
Indolent Systemic Mastocytosis | AB Science | July 1, 2020 | Phase 3 |
NCT04622865 | Recruiting | Drug: Masitinib Drug: Isoquercetin |
SARS-CoV 2 COVID-19 |
AB Science | June 1, 2020 | Phase 2 |
Masitinib inhibition of KIT in intact cells. PLoS One. 2009; 4(9): e7258. td> |
Masitinib inhibits tumour growth in vivo. PLoS One. 2009; 4(9): e7258. |
Effect of masitinib on BCR-ABL and PDGFRα. td> |