Masitinib
Masitinib
CAS: 790299-79-5
Molecular Formula: C28H30N6OS
Masitinib - Names and Identifiers
| Name | Masitinib |
| Synonyms | Ab1010 AB-1010 Ab 1010 AB1010 Ab-1010 AB 1010 Masitinib MASITINIB MASIVET. 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide 4-((4-Methylpiperazin-1-yl)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)-1,3-thiazol-2-yl)amino)phenyl)benzamide 4-[(4-methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)-1,3-thiazol-2-yl]amino}phenyl)benzamide MASITINIB 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide |
| CAS | 790299-79-5 |
| EINECS | 226-164-5 |
| InChI | InChI=1/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) |
Masitinib - Physico-chemical Properties
| Molecular Formula | C28H30N6OS |
| Molar Mass | 498.64 |
| Density | 1.280±0.06 g/cm3(Predicted) |
| Melting Point | 90-95°C |
| Solubility | DMSO 00 mg/mL (200.54 mM);Water <1 mg/mL (<1 mM);Ethanol 4 mg/mL (8.02 mM) |
| Appearance | Solid |
| Color | Off-White to Pale Beige |
| pKa | 13.24±0.70(Predicted) |
| Storage Condition | Refrigerator |
| Refractive Index | 1.682 |
| Use | A tyrosine kinase, c-Kit, PDGFR, FGFR3, the FAK pathway inhibitor. |
| In vitro study | When the concentration of Masitinib is less than or equal to 500 nM, it is a competitive inhibitor of ATP. Masitinib also potently inhibits recombinant PDGFR and the intracellular kinases Lyn, and FGFR 3. However, Masitinib had a weak inhibitory effect on ABL and c-Fms. Masitinib is much more potent than imatinib in inhibiting degranulation, cytokine production, and bone marrow mast cell migration. In Ba/F3 cells expressing human wild-type KIT, Masitinib inhibited SCF (stem cell factor)-induced cell proliferation with an IC50 of 150 nM while inhibiting IL-3-stimulated proliferation, the IC50 value is about> 10 µm. In Ba/F3 cells expressing PDGFR-α, Masitinib inhibited PDGF-BB-stimulated proliferation and PDGFR-α tyrosine phosphorylation with an IC50 of 300 nM. Masitinib acts on mastocytoma cell lines and BMMC and also inhibits stimulated tyrosine phosphorylation of human KIT. Masitinib acts on Ba/F3 cells and inhibits the functional mutations acquired by KIT, including the V559D mutation and the Δ27 mouse mutation, with IC50 of 3 and 5 nM, respectively. Masitinib inhibits cell proliferation in mastocytoma cell lines including HMC-1α155 and FMA3 with IC50 of 10 and 30 nM, respectively. Masitinib acts on two novel ISS cell lines, inhibiting cell growth and PDGFR phosphorylation, indicating that Masitinib inhibits primary and metastatic ISS cell lines and is helpful in the clinical management of ISS. |
| In vivo study | 30 mg/kg Masitinib in the Ba/F3 xenograft tumor model expressing Δ27 inhibited tumor growth and increased medium survival time, with no toxicity to the heart and genes. Daily oral administration of 12.5 mg/kg Masitinib increased overall TTP (tumor growth over time). When combined with Masitinib and gemcitabine inhibited the proliferation of the gemcitabine-resistant cell lines Mia Paca2 and Panc1, they showed a synergistic effect. |
Masitinib - Introduction
Masitinib (AB1010) is a new type of Kit and PDGFRα/β inhibitor. IC50 is 200 nM and 540 nM/800 nM respectively, but it has weak inhibitory effect on ABL and c-Fms. Phase 3
Last Update：2022-10-16 17:28:56
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View History
Masitinib
1-Naphthalenecarboxylic acid, 5-(dimethylamino)-
3-METHYL-6-(TRIFLUOROMETHYL)[1,2,4]TRIAZOLO[4,3-A]PYRIDINE
2-({[4-({[(butylamino)carbonyl]amino}sulfonyl)phenyl]imino}methyl)thiophene
(1-benzyl-3-(hydroxymethyl)pyrrolidin-3-yl)methanol
sodiuM 2-fluoro-3-Methylbenzoate
364597-57-9
145682-85-5
N-(3-bromophenyl)-4-fluorobenzamide
9,10-Epoxyoctadecanoic acid 9,10-epoxyoctadecan-1-yl ester
1-Naphthalenecarboxylic acid, 5-(dimethylamino)-
3-METHYL-6-(TRIFLUOROMETHYL)[1,2,4]TRIAZOLO[4,3-A]PYRIDINE
2-({[4-({[(butylamino)carbonyl]amino}sulfonyl)phenyl]imino}methyl)thiophene
(1-benzyl-3-(hydroxymethyl)pyrrolidin-3-yl)methanol
sodiuM 2-fluoro-3-Methylbenzoate
364597-57-9
145682-85-5
N-(3-bromophenyl)-4-fluorobenzamide
9,10-Epoxyoctadecanoic acid 9,10-epoxyoctadecan-1-yl ester