AB 1010 Mesylate manufacturers
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| | AB 1010 Mesylate Basic information |
| Product Name: | AB 1010 Mesylate | | Synonyms: | AB 1010 Mesylate;AB1010 Mesylate;AB-1010 Mesylate;Masitinib (Mesylate);Masivet Mesylate;Benzamide,4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]-,methanesulfonate;AB1010 MESYLATE; MASIVET MESYLATE; AB-1010 MESYLATE; AB 1010 MESYLATE;AB1010 MESYLATE;AB-1010 MESYLATE;AB 1010 MESYLATE | | CAS: | 1048007-93-7 | | MF: | C29H34N6O4S2 | | MW: | 594.74806 | | EINECS: | | | Product Categories: | | | Mol File: | 1048007-93-7.mol |  |
| | AB 1010 Mesylate Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: ≥ 30 mg/mL (50.44 mM) | | form | Powder | | color | White to yellow | | InChIKey | TXCWBWKVIZGWEQ-UHFFFAOYSA-N | | SMILES | CS(O)(=O)=O.C(NC1=CC=C(C)C(NC2=NC(C3=CC=CN=C3)=CS2)=C1)(=O)C1=CC=C(CN2CCN(C)CC2)C=C1 |
| | AB 1010 Mesylate Usage And Synthesis |
| Uses | Masitinib is a novel tyrosine kinases inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, resectively. | | Uses | Masitinib Mesylate can be used to treat sickle cell disease. | | Synthesis | Synthesis of N-(4-methyl-3-((4-(pyridin-3-yl)thiazol-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide and methanesulfonic acid as 4-[(4-methyl-1-piperazinyl)methyl]-N-(4-methyl-3-((4-(pyridin-3-yl)thiazol-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamidic acid The general procedure for the sulfonate is as follows: 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide (1.0 eq.) was dissolved in ethanol (4.5 v/v), and heated to 65-70°C to dissolve it completely. Under the condition of maintaining the same temperature, methanesulfonic acid (1.0 eq.) was slowly added. Upon completion of the reaction, the mixture was cooled to 25-30 °C and kept at this temperature for 6 hours to promote crystallization. The product was collected by filtration and dried in a vacuum disk dryer at 55-60°C. The yield of this step was 85-90% and the starting melting point of the product was 236°C. | | in vivo | Masitinib inhibits tumour growth and increases the median survival time in Δ27-expressing Ba/F3 tumor models at 30 mg/kg, without cardiotoxicity or genotoxicity[1].
Masitinib (12.5 mg/kg/d, p.o.) increases overall TTP (time-to-tumor progression) compared with placebo in dogs[3]. | | References | [1] Patent: WO2008/98949, 2008, A2. Location in patent: Page/Page column 23 |
| | AB 1010 Mesylate Preparation Products And Raw materials |
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