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Description: Potent and selective Wee1 inhibitor
Chemical Name: 1,2-Dihydro-1-[6-(1-hydroxy-1-methylethyl)-2-pyridinyl]-6-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-2-(2-propen-1-yl)-3H-pyrazolo[3,4-d]pyrimidin-3-one
Purity: ≥98% (HPLC)
Biological Activity for Adavosertib
Adavosertib is a potent and selective Wee1 inhibitor (IC50 = 5.2 nM). In a panel of 223 serine/threonine or tyrosine kinases, Adavosertib is highly selective for Wee 1 over all except 8 kinases. In particular Adavosertib shows >100-fold selectivity over human Myt1. Adavosertib 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 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 synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts.
Technical Data for Adavosertib
| M. Wt | 500.6 |
| Formula | C27H32N8O2 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Adavosertib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.06 | 100 |
Preparing Stock Solutions for Adavosertib
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for Adavosertib
References for Adavosertib
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Adavosertib, please let us know.
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
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Cell Cycle & DNA Damage Repair PosterUpdated
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. Adapted from the 2015 Cancer Product Guide, Edition 3, 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.