Adavosertib
Tocris Bioscience, part of Bio-Techne | Catalog # 7589
Potent and selective Wee1 inhibitor
Key Product Details
Description
Potent and selective Wee1 inhibitor
Alternative Names
AZD 1775,MK 1775
Product Description
Adavosertib 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.Product Specifications
Molecular Weight
500.60
Formula
C27H32N8O2
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 500.60
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.00 mL | 9.99 mL | 19.98 mL |
| 5 mM | 0.40 mL | 2.00 mL | 4.00 mL |
| 10 mM | 0.20 mL | 1.00 mL | 2.00 mL |
| 50 mM | 0.04 mL | 0.20 mL | 0.40 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Lallo 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. 2018 PMID: 29941481
- Hirai MK-1775, a small molecule Wee1 inhibitor, enhances anti-tumor efficacy of various DNA-damaging agents, including 5-fluorouracil. Cancer Biol.Ther. 2010 PMID: 20107315
- Rajeshkumar MK-1775, a potent Wee1 inhibitor, synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts. Clin.Cancer Res. 2011 PMID: 21389100
- Hirai Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents. Mol.Cancer Ther. 2009 PMID: 19887545
Product Specific Notices for Adavosertib
For research use only
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