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说明： Aurora kinase A and B inhibitor
化学名： N-[2-[(1S,4R)-6-[[4-(Cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-acetamide
纯度： ≥98% (HPLC)
生物活性 for PF 03814735
PF 03814735 is an ATP-competitive inhibitor of Aurora kinases A and B (IC50 values are 0.8 and 5 nM for recombinant Aurora B and Aurora A, respectively). Inhibits phosphorylation of Aurora B, histone H3 and Aurora A in cultured MDA-MB-231 cells (IC50 values are approximately 20, 50 and 150 nM respectively). Shown to block cytokinesis; inhibits cellular proliferation in several human tumor cell lines, including HCT-116, HL-60, A549 and H125, and in human xenograft mouse models. Also enhances adeno-associated virus transduction of retina cells in vitro and in vivo. Orally available.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
化合物库 for PF 03814735
PF 03814735 is also offered as part of the Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
技术数据 for PF 03814735
| 分子量 | 474.48 |
| 公式 | C23H25F3N6O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 942487-16-3 |
| PubChem ID | 51346455 |
| InChI Key | RYYNGWLOYLRZLK-RBUKOAKNSA-N |
| Smiles | [H][C@@]3(N5C(CNC(C)=O)=O)CC[C@@]5([H])C(C3=C4)=CC=C4NC1=NC(NC2CCC2)=C(C(F)(F)F)C=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for PF 03814735
参考文献 for PF 03814735
参考文献是支持产品生物活性的出版物。
Jani et al (2010) PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol.Cancer Ther. 9 883 PMID: 20354118
Hook et al (2012) An integrated genomic approach to identify predictive biomarkers of response to the Aurora kinase inhibitor PF-03814735. Mol.Cancer Ther. 11 710 PMID: 22222631
Kollareddy et al (2012) Aurora kinase inhibitors: progress towards the clinic. Invest.New Drugs 30 2411 PMID: 22350019
Maddelena et al (2018) High-throughput screening identifies kinase inhibitors that increase dual adeno-sssociated viral vector transduction in vitro and in mouse retina. Hum.Gene.Ther. 29 886 PMID: 29641320
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关键词: PF 03814735, PF 03814735 supplier, PF03814735, Pfizer, Aurora, kinase, A, B, inhibitors, inhibits, antiproliferative, viral, transduction, enhancer, enhances, Kinases, Viral, Transduction, Enhancers, 4821, Tocris Bioscience
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.