| Description | KPT-251 is a selective nuclear export inhibitor. |
| In vitro | 在对七种患者来源的GBM线[1]的神经球培养进行KPT-251处理时, 显示出剂量响应性的生长抑制。 |
| In vivo | 在系统性转移模型中，通过心内注射PCb2细胞后，80%（8/10）的对照组动物、10%（1/10）接受Selinexor治疗的动物以及20%（2/10）接受KPT-251治疗的动物出现了辐射学证据显示的溶骨性骨损害。同样，在胫骨内注射后，对照组的溶骨区域高于Selinexor和KPT-251组。类似地，血清中破骨细胞标志物（mTRAP和I型胶原片段，CTX）的水平在对照组中显著高于Selinexor和KPT-251治疗组。重要的是，与对照组相比，接受Selinexor和KPT-251治疗的动物的总生存期和无病生存期显著提高。 |
| Synonyms | KPT251 |
| molecular weight | 375.23 |
| Molecular formula | C14H7F6N5O |
| CAS | 1388841-50-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 65 mg/ml (173.23 mM) |
| References | 1. Green AL, et al. Preclinical antitumor efficacy of selective exportin 1 inhibitors in glioblastoma. Neuro Oncol. 2015 May;17(5):697-707. 2. Gravina GL, et al. XPO1/CRM1-selective inhibitors of nuclear export (SINE) reduce tumor spreading and improve overall survival in preclinical models of prostate cancer (PCa). J Hematol Oncol. 2014 Oct 5;7:46. 3. Gravina GL, et al. KPT-330, a potent and selective exportin-1 (XPO-1) inhibitor, shows antitumor effects modulating the expression of cyclin D1 and survivin [corrected] in prostate cancer models. BMC Cancer. 2015 Dec 1;15:941. 4. De Cesare M, et al. Anti-tumor activity of selective inhibitors of XPO1/CRM1-mediated nuclear export in diffuse malignant peritoneal mesothelioma: the role of survivin. Oncotarget. 2015 May 30;6(15):13119-32. |