| 货号:SYN-1092-M001 | 规格:1 mg | 目录价:¥756 |
| 货号:SYN-1092-M005 | 规格:5 mg | 目录价:¥980 |
| 货号:SYN-1092-M010 | 规格:10 mg | 目录价:¥1134 |
| 货号:SYN-1092-M050 | 规格:50 mg | 目录价:¥3332 |
| 货号:SYN-1092-M100 | 规格:100 mg | 目录价:¥询价 |
产品详情
* 以下信息仅供参考,详情请以原厂网站为准
产品名称:
Tozasertib
别名:
MK-0457; VX-680
产品描述:
In mammals, three Aurora kinases, Aurora A, Aurora B, and Aurora C, are expressed. Aurora C expression is mainly restricted to testis, where it functions during meiosis, whereas Aurora A and B play key functions regulating mitosis. Aurora A is localized to the centrosome and spindle poles, where it drives centrosome maturation, separation, and bipolar spindle assembly. Aurora B is the central component of the chromosomal passenger complex (CPC) that also contains the inner centromere protein (INCENP), borealin, and survivin. These non-enzymatic components of the CPC play a key role in regulating kinase activity and localization. Over-expression of Aurora kinases can be oncogeneic and they have thus long been targets for cancer thearpy. Tozasertib, or VX-680, is a potent and selective inhibitor of Aurora kinases, particularly Aurora A and B. In vitro, VX-680 blocks cell cycle progression and induces apoptosis in a wide range of human tumor types at low IC(50) values (i.e. 3.38nM for human BE-13 cells, and 14.34nM for NTERA cells). Moreover, VX680, also has very potent Ki values, with inhibition constants (Ki) of 0.6, 18, and 46nM for Aurora A, B, and C, respectively. VX-680 is also effective in vivo, being used in a Caki-1 xenograft model, VX-680 demonstrated a 75.7% (P < 0.001) decrease in Caki-1 xeno-graft tumor volume with no apparent alternation in animal body weight, peripheral blood counts, or other biological parameters.
保存温度:
+4°C
运输温度:
Ambient
预期分子量:
464.6
产品形式:
solid
产地:
瑞士
纯度:
>95%
CAS号:
639089-54-6
分子式:
C23H28N8OS
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