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Submit ReviewAdavosertib is a potent and selective Wee1 inhibitor (IC50 = 5.2 nM). Blocks CDC2Y15 phosphorylation and Gemcitabine (Cat. No. 3259)-induced DNA damage checkpoint, leading to premature mitotic entry and apoptosis in p53-deficient tumor cell lines. Adavosertib synergizes with gemcitabine to achieve tumor regression in p53-deficient pancreatic cancer xenografts, with Olaparib (Cat. No. 7579) to inhibit SCLC xenograft tumor growth, and inhibits SCLC tumor growth in vivo. Adavosertib also potentiates the cytotoxic effects of Pemetrexed (Cat. No. 6185), Doxorubicin (Cat. No. 2252), Camptothecin (Cat. No. 1100) and Mitomycin C (Cat. No. 3258) in vitro.
Adavosertib is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 500.6 |
公式 | C27H32N8O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 955365-80-7 |
PubChem ID | 24856436 |
InChI Key | BKWJAKQVGHWELA-UHFFFAOYSA-N |
Smiles | O=C1C2=CN=C(N=C2N(C=3N=C(C=CC3)C(O)(C)C)N1CC=C)NC4=CC=C(C=C4)N5CCN(C)CC5 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 50.06 | 100 |
以下数据基于产品分子量 500.6。 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 |
---|---|---|---|
1 mM | 2 mL | 9.99 mL | 19.98 mL |
5 mM | 0.4 mL | 2 mL | 4 mL |
10 mM | 0.2 mL | 1 mL | 2 mL |
50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
参考文献是支持产品生物活性的出版物。
Hirai et al (2009) Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents. Mol.Cancer Ther. 8 2992 PMID: 19887545
Hirai et al (2010) MK-1775, a small molecule Wee1 inhibitor, enhances anti-tumor efficacy of various DNA-damaging agents, including 5-fluorouracil. Cancer Biol.Ther. 9 514 PMID: 20107315
Rajeshkumar et al (2011) MK-1775, a potent Wee1 inhibitor, synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts. Clin.Cancer Res. 17 2799 PMID: 21389100
Lallo et al (2018) The combination of the PARP inhibitor olaparib and the WEE1 inhibitor AZD1775 as a new therapeutic option for small cell lung cancer. Clin.Cancer Res. 24 5153 PMID: 29941481
If you know of a relevant reference for Adavosertib, please let us know.
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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。
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
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.