| Bioactivity | AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity[1][2][3][4][5]. |
| Target | IC50: 2 nM (Eg5) |
| Invitro | AZD4877 (10 nM, 24 or 48 hours) 诱导人膀胱癌细胞凋亡，且对 AZD4877 敏感的细胞通常高表达 p63[2]。 Apoptosis Analysis[2] Cell Line: |
| In Vivo | AZD4877 (静脉注射, 6 或 12 mg/kg；单次) 在大鼠中空纤维模型中，给药后 48 小时使大鼠细胞活力显著降低，裂解的 caspase3 水平增加[1]。AZD4877 (静脉注射, 6 mg/kg；单次)在 Hans Wistar 大鼠中半衰期为 3.5 h，血浆清除率为 36 mL/min/kg[1]。 Animal Model: |
| Name | AZD4877 |
| CAS | 758722-49-5 |
| Formula | C28H33N5O2S |
| Molar Mass | 503.66 |
| 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]. Theoclitou ME, et.al. Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent. J Med Chem. 2011 Oct 13;54(19):6734-50. [2]. Marquis L, et.al. p63 expression correlates with sensitivity to the Eg5 inhibitor ZD4877 in bladder cancer cells. Cancer Biol Ther. 2012 May;13(7):477-86. [3]. Gerecitano JF, et.al. A Phase I trial of the kinesin spindle protein (Eg5) inhibitor AZD4877 in patients with solid and lymphoid malignancies. Invest New Drugs. 2013 Apr;31(2):355-62. [4]. Shahin R, et.al. Kinesin spindle protein inhibitors in cancer: from high throughput screening to novel therapeutic strategies. Future Sci OA. 2022 Feb 21;8(3):FSO778. [5]. Myers SM, et.al. Recent findings and future directions for interpolar mitotic kinesin inhibitors in cancer therapy. Future Med Chem. 2016;8(4):463-89. |