化学性质:
规格 | 10mM * 1 mL in DMSO 5mg 10mg 50mg |
CAS | 942487-16-3 |
别名 | N/A |
化学名 | N/A |
分子式 | C23H25F3N6O2 |
分子量 | 474.48 |
溶解度 | DMF: 20 mg/ml,DMSO: 16 mg/ml,Ethanol: 20 mg/ml,Ethanol:PBS (pH 7.2) (1:9): 0.10 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
PF-03814735 is a potent, orally bioavailable, reversible inhibitor of both Aurora1 and Aurora2 kinases with IC50 values of 0.8nM and 5nM, respectively [1].
PF-03814735 is an ATP competitive inhibitor of Aurora kinases. It also shows inhibition of other protein kinases at 100nM, such as Flt1, FAK, TrkA, Met, and FGFR1. The immunofluorescence imaging analysis shows PF-03814735 can inhibit the phosphorylation of Aurora1, Aurora 2 as well as histone H3 in MDA-MB-231 cells. This inhibition is rapid and reversible. The inhibition of phosphorylated histone H3 also occurs in athymic mice bearing HCT-116 xenografts. PF-03814735 induces the formation of polyploid cells and multinucleated cells due to the block in cytokinesis secondary. Moreover, PF-03814735 treatment results in a reduction of cell proliferation in vitro (such as HL-60, A549, and H125) and a inhibition of tumor growth in vivo (human xenograft mouse models, such as A2780 ovarian carcinoma and HCT-116) [1].
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标签:PF-03814735
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