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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.
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Application | oral gavage |
| Results | Asterisk indicates those models that had a significant difference in tumour progression for the AZD1775 + IRN + VCR relative to IRN + VCR. |
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Application | oral gavage |
| Results | The mice treated with AZD1775 + VCR + IRN had a better response than those treated with VCR + IRN alone. |
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Application | Targeting the G2/M |
| 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. |
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Application | Targeting the G2/M |
| Results | Sustained levels of GSP and AZD1775 in tumors were above those required to potentiate cytotoxic effects in culture. |
| 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. |
| 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 |
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RP-6306 (Lunresertib) is the first-in-class, highly potent and selective PKMYT1 inhibitor that preferentially kills tumor cells overexpressing CCNE1 and was shown to inhibit the growth of a broad range of CCNE1-amplified tumors in xenograft/PDX preclinical models, both as a single agent and in combination therapy settings. |
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WEE1-IN-5 is a potent WEE1 inhibitor with an IC50 value of 0.8 nM. WEE1-IN-5 inhibits phospho-CDC2. WEE1-IN-5 abrogates the G2 check point, increasing sensitivity to DNA damaging agents in cancer cells. |
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