Tirbanibulin Mesylate (KX2-391 Mesylate) 是一种有效的 Src 抑制剂，在肿瘤细胞中，GI₅₀ 值为 9-60 nM。

Tirbanibulin Mesylate (KX2-391 Mesylate) is an inhibitor of Src that targets the peptide substrate site of Src, with GI 50 of 9-60 nM in cancer cell lines.

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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)

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. has not independently confirmed the accuracy of these methods.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

[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.

In Vitro: DMSO : 100 mg/mL (189.53 mM; Need ultrasonic)配制储备液