S81899 |
KX2-391 (Mesylate) |
| 源叶(MedMol) | 99% |
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- 产品描述： 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
- 靶点： GI50: 9 nM (Src, in HuH7 cells), 13 nM (Src, in PLC/PRF/5 cells), 26 nM (Src, in Hep3B cells), 60 nM (Src, in HepG2 cells)
- 体外研究：
Tirbanibulin Mesylate (KX2-391 Mesylate) 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. Tirbanibulin Mesylate (KX2-391 Mesylate) 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 Mesylate (KX2-391 Mesylate) 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
- 体内研究：
Orally administered Tirbanibulin Mesylate (KX2-391 Mesylate) is shown to inhibit primary tumor growth and to suppress metastasis, in pre-clinical animal models of cancer
- 参考文献：
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.
- 溶解性： soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.895 ml 9.476 ml 18.953 ml 5 mM 0.379 ml 1.895 ml 3.791 ml 10 mM 0.19 ml 0.948 ml 1.895 ml 50 mM 0.038 ml 0.19 ml 0.379 ml
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