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Tirbanibulin dihydrochloride

CAS No. : 1038395-65-1

MCE 国际站：Tirbanibulin dihydrochloride

产品活性：Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) 是 Src 的抑制剂，在肿瘤细胞中，GI₅₀ 值为 9-60 nM。

研究领域：Protein Tyrosine Kinase/RTK  |  Cytoskeleton  |  Cell Cycle/DNA Damage

作用靶点：Src  |  Microtubule/Tubulin

In Vitro: Tirbanibulin (KX2-391) is a Src inhibitor that is directed to the Src substrate pocket. 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 (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.

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

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