Adavosertib

Name: Adavosertib
Brand: Tocris Bioscience
SKU: 7589

Tocris Bioscience, part of Bio-Techne | Catalog # 7589

Citations (1)

COA / SDS

Potent and selective Wee1 inhibitor

Key Product Details

Description:	Potent and selective Wee1 inhibitor
Alternative Names:	AZD 1775,MK 1775
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)
Molecular Weight:	500.6

View Full Technical Details for Adavosertib

Technical Data
Citations

Biological Activity for Adavosertib

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.

Compound Libraries for Adavosertib

Adavosertib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

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 for Adavosertib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	2.00 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

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Reconstitution Calculator

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References for Adavosertib

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