Lexibulin (CYT-997) 是微管蛋白聚集强效抑制剂，对多种癌细胞的 IC50 值为 10-100n M，体外体内具有高效的细胞毒性和血管增生阻断作用。Lexibulin 可诱导细胞凋亡 (apoptosis)，并诱导 GC 细胞中的线粒体 ROS 生成。

Lexibulin (CYT-997) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin induces cell apoptosis and induces mitochondrial ROS generation in GC cells.

Solid

IC50 value: 10-100 nM(cell assay)

Lexibulin (CYT-997) prevents the in vitro polymerization of tubulin with an IC50 of ～3 μmol/L (compared with the half-maximal inhibitory concentration of 2 μmol/L for colchicine under identical conditions) as determined using the conventional turbidimetric assay for tubulin polymerization. Lexibulin is also capable of reversibly disrupting the microtubule network in cells, visualized using fluorescence microscopy. Thus, treatment of A549 cells with Lexibulin (1 μM) lead to the rapid reorganization of microtubules, including the destruction of the existing microtubule network and accumulation of tubulin in plaques within the cytoplasm of some cells. After 24 hours, major alterations in cell morphology are evident, including loss of adhesion and cell rounding. The effect of 1 hour of treatment with Lexibulin is reversible and cells rapidly recovered their normal microtubule arch

iIn a xenograft model using the human prostate cancer cell line PC3, oral dosing of Lexibulin (CYT-997) is initiated 13 days after cell implantation by which time palpable tumors were evident. A dose-dependent inhibition of tumor growth was apparent with Lexibulin (CYT-997), which at the highest dose was equivalent to parenterally administered paclitaxel. A single dose of Lexibulin (CYT-997) (7.5 mg/kg i.p.) clearly decreased blood flow in liver metastases, and a significant reduction in blood flow was present 6 hours postdose. Lexibulin (CYT-997) treatment (15 mg/kg/day) significantly prolongs the survival in a murine model of aggressive systemic myelomatosis. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Burns CJ, et al. CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Mol Cancer Ther. 2009 Nov;8(11):3036-45.
[2]. Monaghan K, et al. CYT997 causes apoptosis in human multiple myeloma. Invest New Drugs. 2011 Apr;29(2):232-8.

In Vitro: DMSO : ≥ 100 mg/mL (230.13 mM)配制储备液