Tirbanibulin Mesylate 是一种 Src 抑制剂,靶向 Src 的肽底物位点。在肿瘤细胞中,GI50值为 9-60 nM。
半岛bd体育手机客户端 描述
Tirbanibulin Mesylate is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).
体外活性
Tirbanibulin 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 displays 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 Mesylate is evaluated in engineered Src drove cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively [2].
体内活性
In pre-clinical animal models of cancer, Tirbanibulin Mesylate (p.o.) is shown to inhibit primary tumor growth and to suppress metastasis [2].
Cas No.
1080645-95-9
分子式
C27H33N3O6S
分子量
527.63
别名
KX01 Mesylate;KX2-391 Mesylate
储存和溶解度
DMSO:99 mg/mL (187.63 mM,Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years