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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
CC1=CC=C(NC(C2=CC=C(CN3CCN(C)CC3)C=C2)=O)C=C1NC4=NC(C5=CN=CC=C5)=CS4
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)
InChI 密鑰
WJEOLQLKVOPQFV-UHFFFAOYSA-N
生化／生理作用
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.
訊號詞
Warning
危險聲明
危險分類
Acute Tox. 4 Oral - Repr. 2 - STOT RE 2
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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)
Masitinib, a c-kit/PDGF receptor tyrosine kinase inhibitor, improves disease control in severe corticosteroid-dependent asthmatics
M Humbert
Allergy, 64, 1194-1201 (2009)
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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