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Submit ReviewBAY 1816032
说明： Potent and selective BUB1 kinase inhibitor
化学名： 2-[3,5-Difluoro-4-[[3-[5-methoxy-4-[(3-methoxy-4-pyridinyl)amino]-2-pyrimidinyl]-1H-indazol-1-yl]methyl]phenoxy]ethanol
纯度： ≥98% (HPLC)
生物活性 for BAY 1816032
BAY 1816032 is a potent and selective inhibitor of BUB1 kinase, a mitotic checkpoint serine/threonine kinase (IC50 = 6.1 nM). BAY 1816032 shows 17-fold selectivity over a panel of 403 other human kinases. In vivo, BAY 1816032 decreases tumor size in tumor xenograft models. BAY 181603 is orally bioavailable.
化合物库 for BAY 1816032
BAY 1816032 is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
技术数据 for BAY 1816032
| 分子量 | 534.52 |
| 公式 | C27H24F2N6O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1891087-61-8 |
| PubChem ID | 118958833 |
| InChI Key | QVOGVAVHOLLLAZ-UHFFFAOYSA-N |
| Smiles | COC1=CN=C(N=C1NC2=C(C=NC=C2)OC)C3=NN(C4=CC=CC=C43)CC5=C(C=C(C=C5F)OCCO)F |
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.
溶解性数据 for BAY 1816032
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 26.73 | 50 |
制备储备液 for BAY 1816032
以下数据基于产品分子量 534.52。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.74 mL | 18.71 mL | 37.42 mL |
| 2.5 mM | 0.75 mL | 3.74 mL | 7.48 mL |
| 5 mM | 0.37 mL | 1.87 mL | 3.74 mL |
| 25 mM | 0.07 mL | 0.37 mL | 0.75 mL |
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产品说明书 for BAY 1816032
参考文献 for BAY 1816032
参考文献是支持产品生物活性的出版物。
Siemeister et al (2019) Inhibition of BUB1 kinase by BAY 1816032 sensitizes tumor cells toward taxanes, ATR, and PARP inhibitors in vitro and in vivo. Clin.Cancer Res. 25 1404 PMID: 30429199
If you know of a relevant reference for BAY 1816032, please let us know.
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关键词: BAY 1816032, BAY 1816032 supplier, BAY1816032, BUB1, kinases, inhibitors, inhibits, mitotic, mitosis, potent, selective, xenograft, tumor, serine/threonine, checkpoint, Mitosis, Checkpoint, Control, Kinases, 7549, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
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.