性能参数

产品名称

Masitinib (AB1010)

规格

10mg 25mg 100mg

货号

GOY-Y3175

 含量

>98.00%

CAS

790299-79-5

别名

化学名

4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-yl-1,3-thiazol-2-yl)amino]phenyl]benzamide

分子式

C28H30N6OS

分子量

分子量 498.64

溶解度

≥ 24.95mg/mL in DMSO

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

The stem cell factor receptor (KIT) is a therapeutic target for the cancer, mastocytosis, and inflammatory diseases treatment. Masitinib (AB1010) is a novel phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT.

In vitro: Masitinib potently inhibited the intracellular kinase Lyn and recombinant PDGFR as well as fibroblast growth factor receptor 3. Moreover, masitinib showed weak inhibition of ABL and c-Fms and was inactive against a variety of other tyrosine and serine/threonine kinases. These findings suggest that Masitinib (AB1010) will exhibit a better safety profile than other tyrosine kinase inhibitors; in fact, masitinib-induced genotoxicity or cardiotoxicity has not been observed in animal so far [1].

In vivo: In vivo, masitinib blocked tumour growth in mice with subcutaneous grafts of Ba/F3 cells expressing a juxtamembrane KIT mutant. We found that tumour growth was blocked following 5 days of treatment with masitinib. After withdrawal of masitinib treatment after day 5, tumour growth was once again evident [1].

Clinical trial: A Phase II study of oral masitinib mesilate in imatinib-na?ve patients with locally advanced or metastatic gastro-intestinal stromal tumour (GIST). Thirty patients were enrolled with a median follow-up of 34 months. Masitinib appears to be effective as a first-line treatment of advanced GIST with comparable results to imatinib in terms of safety and response. PFS and OS results data show promise that masitinib may provide sustainable benefits [2].

利多卡因  137-58-6  硝酸镱  13768-67-7

缬沙坦烃化物  137863-89-9  6,7-二甲氧基喹唑啉-4-酮  13794-72-4

2,5-二氯-3-溴吡啶  138006-41-4  4-溴-3-甲基吡唑  13808-64-5

三水氯化钌  13815-94-6  氯钯酸钠  13820-53-6

硅烷偶联剂 KH-540  13822-56-5  3-苯氧基苄醇  13826-35-2

对磺酰胺苯甲酸  138-41-0  水杨甙  138-52-3

CCK-B Receptor Antagonist 25mg 10mg 50mg 100mg>98.50%Cas No. 155412-88-7C27H28N6O3

Azeliragon5mg 10mg 50mg 100mg 200mg>98.50%Cas No. 603148-36-3C32H38ClN3O2

Columbin10mM*1mLinDMSO 5mg 10mg 25mg 50mg>98.50%Cas No. 546-97-4C20H22O6

Devazepide10mM (in 1mL DMSO) 5mg 10mg 25mg 50mg 100mg>98.50%Cas No. 103420-77-5C25H20N4O2

Decloxizine dihydrochloride10mM*1mL in DMSO 50mg 100mg 500mg 1g 5g>98.50%Cas No. 13073-96-6C21H30Cl2N2O2

>

Betazole10 mg 50 mg>96.00%Cas No. 105-20-4C5H9N3