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MK 1775
- AZD 1775 - Adavosertib
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C27H32N8O2
- MW: 500.6
Description
MK 1775 is adavosertib (AZD1775), a potent inhibitor of the checkpoint kinase WEE1. Inhibition of WEE1 reduces inhibitory Tyr15 phosphorylation of CDK1 and CDK2, forcing cell-cycle progression despite DNA damage or incomplete DNA replication.
By abrogating the G2/M and replication-stress checkpoints, MK 1775 can increase the cytotoxicity of DNA-damaging agents and is especially useful in models that rely heavily on the WEE1 checkpoint, including many TP53-deficient cancers.
Key Features
- Potent WEE1 kinase inhibitor
- Reduces inhibitory CDK1/CDK2 Tyr15 phosphorylation
- Abrogates DNA-damage and replication-stress checkpoints
- Sensitizes checkpoint-dependent tumor cells to genotoxic stress
Applications
- WEE1 and cell-cycle checkpoint research
- DNA-damage response and replication-stress studies
- Combination studies with chemotherapy or radiation
- TP53-deficient and checkpoint-dependent cancer models
More Information
| Parent CAS No. | 955365-80-7 |
|---|---|
| Chemical Name | 2-Allyl-1-[6-(1-hydroxy-1-methyl-ethyl)-pyridin-2-yl]-6-[4-(4-methyl-piperazin-1-yl)-phenylamino]-1,2-dihydro-pyrazolo[3,4-d]pyrimidin-3-one |
| SMILES | C1(NC2C=CC(N3CCN(C)CC3)=CC=2)=NC2N(C3C=CC=C(C(O)(C)C)N=3)N(CC=C)C(=O)C=2C=N1 |
| MFCD | MFCD17215200 |
| InChi | InChI=1S/C27H32N8O2/c1-5-13-34-25(36)21-18-28-26(29-19-9-11-20(12-10-19)33-16-14-32(4)15-17-33)31-24(21)35(34)23-8-6-7-22(30-23)27(2,3)37/h5-12,18,37H,1,13-17H2,2-4H3,(H,28,29,31) |
| InChiKey | BKWJAKQVGHWELA-UHFFFAOYSA-N |
| CID | 24856436 |
| Short Description | Wee1 inhibitor |
References
- H. Hirai et al. Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents. Mol. Cancer. Ther. 2009, 8(11), 2992-3000.
- S. Schellens et al. A Phase I and pharmacological study of MK-1775, a Wee1 tyrosine kinase inhibitor, in both monotherapy and in combination with gemcitabine, cisplatin, or carboplatin in patients with advanced solid tumors. J. Clin. Oncol. 2009, 27.
- H. Hirai et al. MK-1775, a small molecule Wee1 inhibitor, enhances anti-tumor efficacy of various DNA-damaging agents, including 5-fluorouracil. Cancer Biol. Ther. 2010, 9(7), 523-525.
- CC Porter et al. Integrated genomic analyses identify WEE1 as a critical mediator of cell fate and a novel therapeutic target in acute myeloid leukemia. Leukemia 2012, 26, 1266-1276.
- List of publications using MK 1775 (Axon 1494) purchased from Axon Medchem
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