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CAS No.: 398493-79-3

PHA-680632 Catalog No. CSN12811

Synonyms: PHA-680632

PHA-680632 is potent inhibitor of Aurora A, B and C with IC50 of 27 nM, 135 nM and 120 nM, respectively.

规格	价格	促销价格	库存	数量

400-920-2911

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实验方案

技术信息

生物活性

描述Aurora proteins belong to a small family of serine/threonine kinases, including three members: Aurora A, Aurora B, and the less well characterized Aurora C, that regulate the structure and function of the cytoskeleton and chromosomes and the interactions between these two at the kinetochore. They also regulate signalling by the spindle-assembly checkpoint pathway and cytokinesis. Perturbation of Aurora kinase expression or function might lead to cancer^[3]. PHA-680632 is a novel, highly selective Aurora kinase inhibitor, with three Aurora kinases with IC₅₀s of 27, 135 and 120 nM for Aurora A, B, and C respectively, that inhibits the phosphorylation of Histone H3 in Ser10, which is mediated by Aurora B kinase. In a vitro study, C33A, HeLa, HCT116, HT29 cell lines were treated with PHA-680632 and incubated for 72 hours. It indicates that PHA-680632 is a efficient cell cycle inhibitor with IC₅₀ values of 0.32 μM, 0.41 μM, 0.06 μM and 1.17 μM for C33A, HeLa, HCT116, HT29 cell lines respectively. In a vivo study, A2780 human ovarian carcinoma and HCT116 colon carcinoma cell lines were transplanted s.c. into athymic mice. In the A2780 human ovarian carcinoma model, the dose of 60 mg/kg i.v. b.i.d. for 5 days showed potent tumor inhibition, reaching 78% of TGI compared with the vehicle-treated controls. A more prolonged exposure to PHA-680632 was tested in the HCT116 colon carcinoma xenograft, administering the compound i.p. t.i.d. for 12 days. The treatments were also in this case well tolerated and TGI was 75% compared with controls^[3].
作用机制PHA-680632 inhibit autophosphorylation at Thr248 in the activation loop and process of binding to the CPC protein INCENP^[4].
动物研究
剂量
Mice: 15 mg/kg - 45 mg/kg^[2] (i.v., BID); 40 mg/kg^[1] (i.p., BID)

给药途径
i.v., i.p.
参考文献

动物研究
剂量	Mice: 15 mg/kg - 45 mg/kg^[2] (i.v., BID); 40 mg/kg^[1] (i.p., BID)
给药途径	i.v., i.p.

[1] Tao Y, Zhang P, et al. Enhancement of radiation response by inhibition of Aurora-A kinase using siRNA or a selective Aurora kinase inhibitor PHA680632 in p53-deficient cancer cells. Br J Cancer. 2007 Dec 17;97(12):1664-72.
[2] Soncini C, Carpinelli P, et al. PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity. Clin Cancer Res. 2006 Jul 1;12(13):4080-9.
[3] Soncini C, Carpinelli P, Gianellini L, Fancelli D, Vianello P, Rusconi L, Storici P, Zugnoni P, Pesenti E, Croci V, Ceruti R, Giorgini ML, Cappella P, Ballinari D, Sola F, Varasi M, Bravo R, Moll J. PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity. Clin Cancer Res. 2006 Jul 1;12(13):4080-9.
[4] Pollard JR, Mortimore M. Discovery and development of aurora kinase inhibitors as anticancer agents. J Med Chem. 2009 May 14;52(9):2629-51.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9935 mL
- 9.9676 mL
- 19.9353 mL
- 5 mM
- 0.3987 mL
- 1.9935 mL
- 3.9871 mL
- 10 mM
- 0.1994 mL
- 0.9968 mL
- 1.9935 mL

技术信息

CAS号

398493-79-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H35N7O2

运输

蓝冰

分子量

501.62

别名

PHA-680632

溶解度

DMSO	550.0 mg/mL (1096.4 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	11 mg/mL	clear
PO	0.5% CMC-Na	43 mg/mL	suspension

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