S80697 |
PHA-680632 |
源叶(MedMol) | 98% |
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- 产品描述: PHA-680632 is an aurora kinase inhibitor with IC50s of 27, 135 and 120 nM for aurora A, B and C, respectively.
- 靶点: Aurora A:27 nM (IC50);Aurora B:135 nM (IC50);Aurora C:120 nM (IC50);FGFR;PLK;AuroraKinase
- 体内研究:
PHA-680632 suppresses tumor growth in animal models. PHA-680632 treatment at 45 mg/kg dose results in 85% of TGI without signs of toxicity in the HL60 human acute myelogenous leukemia xenograft model. PHA-680632 treatment at 60 mg/kg i.v. b.i.d. for 5 days results in 78% of TGI without signs of toxicity in the A2780 human ovarian carcinoma model. PHA680632 in association with radiation leads to an additive effect in cancer cells, especially in the p53-deficient cells, but does not act as a radiosensitiser
- 参考文献:
1. Soncini C, et al. PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity. Clin Cancer Res. 2006 Jul 1;12(13):4080-9. 2. Tao Y, 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.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.993 ml 9.967 ml 19.935 ml 5 mM 0.399 ml 1.993 ml 3.987 ml 10 mM 0.199 ml 0.997 ml 1.993 ml 50 mM 0.04 ml 0.199 ml 0.399 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)