货号 | 3728/50 |
别名 | 2-[1-(4-Chlorobenzyl)-1H-indol-3-yl |
供应商 | Tocris |
生物活性 | Microtubule destabilizer that blocks tubulin polymerization (IC50 = 0.3 μM). Blocks cell cycle progression at metaphase and displays antitumor activity against a variety of malignancies in vitro(IC50 values ranging from 0.036 - 0.285 μM). Induces complete tumor remission in the Yoshida AH13 rat sarcoma model in vivo. Lacks neurotoxicity due to an ability to discriminate between posttranslationally modified tubulin in mature neuronal microtubules and less-modified tubulin present in immature neuronal or nonneuronal microtubules. Displays oral availability and efficacy towards MDR tumor cells. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 389.83 |
分子式 | C22H16CIN3O2 |
可溶性/溶解性 | Soluble to 25 mM in DMSO |
CAS号 | 204205-90-3 |
参考文献 | Wienecke and Bacher (2009) Indibulin, a novel microtubule inhibitor, discriminates between mature and nonneuronal tubulin. Cancer Res. 69 171. PMID: 19118000. Kanzawaet al (2005) Microtubule inhibitor D-24851 induces p53-independent apoptotic cell death in malignant glioma cells through Bcl-2 phosphorylation and Bax translocation. Int.J.Oncol. 26 589. PMID: 15703812. Bacheret al (2001) D-24851, a novel synthetic microtubule inhibitor, exerts curative antitumoral activity in vivo, shows efficacy toward multidrug-resistant tumor cells, and lacks neurotoxicity. Cancer Res. 61 392. PMID: 11196193. |