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Adavosertib (MK-1775)

Cat. No. M2143

All AbMole products are for research use only, cannot be used for human consumption.

Adavosertib (MK-1775) Structure
Synonym:

AZD1775

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 45  USD45 In stock
5mg USD 40  USD40 In stock
10mg USD 65  USD65 In stock
25mg USD 75  USD75 In stock
50mg USD 95  USD95 In stock
500mg USD 285  USD285 In stock
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Quality Control & Documentation
Biological Activity

Adavosertib (AZD1775, MK-1775) is a small pyrazolacil derivative, an effective ATP competitive specific inhibitor of WEE1 kinase, with IC50 of 5.2 nM. It can inhibit G2 phase DNA damage test sites. MK-1775 (Adavosertib) inhibits phosphorylation of CDC2 at Tyr15 (CDC2Y15), a direct substrate of Wee1 kinase in cells.

Product Citations
Customer Product Validations & Biological Datas
Source Cancer Cell (2018). Figure 8. AZD1775 (Abmole Bioscience, Houston, USA)
Method Targeting the G2/M
Cell Lines RMS cell lines
Concentrations 1 uM
Incubation Time 24 or 48 hr
Results Sustained levels of GSP and AZD1775 in tumors were above those required to potentiate cytotoxic effects in culture.
Source Cancer Cell (2018). Figure 7. AZD1775 (Abmole Bioscience, Houston, USA)
Method Targeting the G2/M
Cell Lines RMS cell lines
Concentrations 1 uM
Incubation Time 24 or 48 hr
Results AZD1775 combined with IRN or VCR led to high rates of DNA damage (Figure 7G), suggesting that both WEE1 and HSP90 may be druggable targets in RMS.
Source Nature (2017). Figure 6. AZD1775 (Abmole Bioscience)
Method oral gavage
Cell Lines Athymic nude immunodeficient mice
Concentrations 60 mg/kg
Incubation Time 1–5 days
Results The mice treated with AZD1775 + VCR + IRN had a better response than those treated with VCR + IRN alone.
Source Nature (2017). Figure 4. AZD1775 (Abmole Bioscience)
Method oral gavage
Cell Lines Athymic nude immunodeficient mice
Concentrations 60 mg/kg
Incubation Time 1–5 days
Results Asterisk indicates those models that had a significant difference in tumour progression for the AZD1775 + IRN + VCR relative to IRN + VCR.
Protocol (for reference only)
Cell Experiment
Cell lines WiDr and H1299 cells
Preparation method Cell Viability Assay.
Cells were seeded in 96-well plates and treated with gemcitabine for 24 h, then with MK-1775 for an additional 24 h. Cell viability was determined with a WST-8 kit using SpectraMax (Molecular Devices).
Concentrations 0, 30, 100 and 300 nM
Incubation time 24 h
Animal Experiment
Animal models nude rats bearing WiDr Subcutaneous xenograft tumors
Formulation 0.5% methylcellulose solution
Dosages 20mg/kg
Administration p.o.
Chemical Information
Molecular Weight 500.61
Formula C27H32N8O2
CAS Number 955365-80-7
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Bridges KA, et al. Clin Cancer Res. MK-1775, a novel Wee1 kinase inhibitor, radiosensitizes p53-defective human tumor cells.

[2] Rajeshkumar NV, et al. Clin Cancer Res. MK-1775, a potent Wee1 inhibitor, synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts.

[3] Hirai H, et al. Cancer Biol Ther. MK-1775, a small molecule Wee1 inhibitor, enhances anti-tumor efficacy of various DNA-damaging agents, including 5-fluorouracil.

[4] Hirai H, et al. Mol Cancer Ther. Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents.

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Keywords: Adavosertib (MK-1775), AZD1775 supplier, Wee1, inhibitors, activators

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