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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.
Cancer Cell. 2018 Sep 10;34(3):411-426.e19.
Identification of Therapeutic Targets in Rhabdomyosarcoma through Integrated Genomic, Epigenomic, and Proteomic Analyses.
Adavosertib (MK-1775) purchased from AbMole
Nature. 2017 Sep 7;549(7670):96-100.
Orthotopic patient-derived xenografts of paediatric solid tumours
Adavosertib (MK-1775) purchased from AbMole
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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. |
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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. |
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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. |
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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. |
| 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 |
| Related Wee1 Products |
|---|
| WEE1-IN-5
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. |
| WEE1-IN-4
WEE1-IN-4 is a potent checkpoint Wee1 kinase inhibitor with an IC50 of 0.011 μM. |
| Pomalidomide-C3-adavosertib
Pomalidomide-C3-adavosertib is a rapid and selective Wee1 degrader (IC50=3.58 nM). Pomalidomide-C3-adavosertib shows anti-cancer cell proliferation activity, and induces apoptosis. |
| PD0166285 dihydrochloride
PD0166285 dihydrochloride, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC50 of 3.433 μM for Chk1. |
| RP-6306
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. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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