| Bioactivity | KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell[1]. |
| Invitro | KX2-361 (0-200 nM，24-72 小时)可降低 GL261 细胞中 Src 的自身磷酸化[1]。KX2-361 (0-270 nM) 促进 U87 细胞的细胞周期停滞在 G2/M 期。注意 270 nM 时的剂量依赖性效应完全停止[1]。KX2-361 (0-800 nM) 诱导 U87、GL261 和 T98G 细胞系凋亡[1]。KX2-361 (5 µM) 抑制微管蛋白聚合物的体外组装[1]。 0 --> KX2-361 相关抗体: |
| In Vivo | KX2-361 显著延缓原位 GL261 脑肿瘤的进展并实现长期生存[1]。当给小鼠口服给药(20 mg/kg)时，KX2-361表现出明显的脑渗透性，给药后15分钟观察到的脑Cmax为4025±319 ng/g，总暴露（AUClast）为5044±355 h ng/ g[1]。 |
| Name | KX2-361 |
| CAS | 897016-26-1 |
| Formula | C24H24FN3O2 |
| Molar Mass | 405.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ciesielski MJ, et al. KX2-361: a novel orally bioavailable small molecule dual Src/tubulin inhibitor that provides long term survival in a murine model of glioblastoma. J Neurooncol. 2018 Dec;140(3):519-527. |