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Merck
CN

SML3594

Masitinib

≥98% (HPLC)

别名:

4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]-benzamide, AB1010

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关于此项目

经验公式(希尔记法):
C28H30N6OS
化学文摘社编号:
分子量:
498.64
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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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)

SMILES string

CC1=CC=C(NC(C2=CC=C(CN3CCN(C)CC3)C=C2)=O)C=C1NC4=NC(C5=CN=CC=C5)=CS4

InChI key

WJEOLQLKVOPQFV-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

Biochem/physiol Actions

Masitinib is a protein tyrosine kinase inhibitor that selectively targets stem cell factor receptor c-kit in particular and also PDGFRalpha/beta and Lyn. It is more potent and selective for c-kit than imatinib (Gleevec). Masitinib has antineoplastic and anti-inflammatory activity. It inhibits the survival, migration and activity of mast cells, key components of the inflammation response. It is used to treat mast cell tumors in dogs and is in clinical trials for human use in rheumatoid arthritis, asthma, and as an adjuct therapy for Alzheimer′s disease.
c-kit/PDGF receptor tyrosine kinase inhibitor

pictograms

Health hazardExclamation mark

signalword

Warning

Hazard Classifications

Acute Tox. 4 Oral - Repr. 2 - STOT RE 2

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Masitinib, a c-kit/PDGF receptor tyrosine kinase inhibitor, improves disease control in severe corticosteroid-dependent asthmatics
M Humbert
Allergy, 64, 1194-1201 (2009)
Masitinib as an adjunct therapy for mild-to-moderate Alzheimer's disease: a randomised, placebo-controlled phase 2 trial
Francois Piette
Alzheimer's Research & Therapy, 3, 16-16 (2011)
Patrice Dubreuil et al.
PloS one, 4(9), e7258-e7258 (2009-10-01)
The stem cell factor receptor, KIT, is a target for the treatment of cancer, mastocytosis, and inflammatory diseases. Here, we characterise the in vitro and in vivo profiles of masitinib (AB1010), a novel phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT.

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