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Tirbanibulin Mesylate(KX2-391(Mesylate))
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tirbanibulin Mesylate(KX2-391(Mesylate))图片
CAS NO:1080645-95-9
规格:98%
分子量:527.63
包装与价格:
包装价格(元)
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Tirbanibulin(Mesylate)(KX2-391(Mesylate))是一种有效的Src抑制剂,在肿瘤细胞中,GI50值为9-60nM。
CAS:1080645-95-9
分子式:C27H33N3O6S
分子量:527.63
纯度:98%
存储:Store at -20°C

Background:

Tirbanibulin (Mesylate) (KX2-391 (Mesylate)) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.


Tirbanibulin (KX2-391) is a Src inhibitor that is directed to the Src substrate pocket. Tirbanibulin (KX2-391) shows steep dose-response curves against Huh7 (GI50=9 nM), PLC/PRF/5 (GI50=13 nM), Hep3B (GI50=26 nM), and HepG2 (GI50=60 nM), four hepatic cell cancer (HCC) cell lines[1]. Tirbanibulin (KX2-391) is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. Tirbanibulin (KX2-391) is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively[2].


Orally administered Tirbanibulin (KX2-391) is shown to inhibit primary tumor growth and to suppress metastasis, in pre-clinical animal models of cancer[2].


[1]. Lau GM, et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. Dig Dis Sci, 2009, 54(7), 1465-1474. [2]. Fallah-Tafti A, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities. Eur J Med Chem, 2011, 46(10), 4853-4858.


 
 
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