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Lexibulin dihydrochloride

产品编号 T15746 CAS 917111-49-0

别名: CYT-997 dihydrochloride

Lexibulin 2Hcl is an effective tubulin polymerization inhibitor (IC50: 10-100 nM in cancer cell lines). It also has potent cytotoxic and vascular disrupting activity in vitro and in vivo.

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Lexibulin dihydrochloride Chemical Structure

Lexibulin dihydrochloride, CAS 917111-49-0

规格	价格/CNY	货期
25 mg	￥ 10,600	6-8周
50 mg	￥ 13,800	6-8周
100 mg	￥ 17,500	6-8周

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Lexibulin dihydrochloride 的其他形式现货产品:

Lexibulin

其他形式的 Lexibulin dihydrochloride:

Lexibulin
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Lexibulin 2Hcl is an effective tubulin polymerization inhibitor (IC50: 10-100 nM in cancer cell lines). It also has potent cytotoxic and vascular disrupting activity in vitro and in vivo.
靶点活性	Tubulin polymerization:10-100 nM
体外活性	CYT997 was also capable of reversibly disrupting the microtubule network in cells, visualized using fluorescence microscopy. Thus, the treatment of A549 cells with CYT997 (1 μmol/L) leads 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. CYT997 prevented the in vitro polymerization of tubulin (IC50: ～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. Only 66% of total cells were in the G1, S, and G2-M phases, at 24 hours post-CYT997 treatment, which shows that cells blocked at the G2-M boundary do not exit back to G1, as in the normal cell cycle, but most likely are driven towards apoptosis and cell death [1]. CYT997 potently inhibits proliferation, consistent with the disruption of cellular tubulin, induces cell cycle arrest, and most importantly apoptosis of both human myeloma cell lines (HMCLs) and primary MM cells [2]. Major alterations in cell morphology were evident, after 24 hours, including loss of adhesion and cell rounding. The effect of 1 hour of treatment with CYT997 was reversible and cells rapidly recovered their normal microtubule architecture. The data indicate that CYT997 belongs to the class of anticancer agents that disrupt, rather than stabilize, tubulin-containing structures. Although vehicle-treated cells show 15% and 19% in G2-M phase at 15 and 24 hours (respectively), cells treated with CYT997 (1 μmol/L) had 38% and 43% of cells in G2-M at the same time points.
体内活性	A single dose of CYT997 (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 [1]. CYT997 treatment (15 mg/kg/day) significantly prolongs the survival in a murine model of aggressive systemic myelomatosis [2]. In a xenograft model using the human prostate cancer cell line PC3, oral dosing of CYT997 was initiated 13 days after cell implantation by which time palpable tumors were evident. Dose-dependent inhibition of tumor growth was apparent with CYT997, which at the highest dose was equivalent to parenterally administered paclitaxel.

别名	CYT-997 dihydrochloride
分子量	507.46
分子式	C24H32Cl2N6O2
CAS No.	917111-49-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

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.

剂量换算

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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