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Background Information:
MK-1775 (Adavosertib) (AZD1775) is an orally bioavailable, clinical stage, small molecule inhibitor of Wee1, a kinase that phosphorylates CDC2 to inactivate the CDC2/cyclin B complex (regulating the G2 checkpoint). Since most human cancers harbor p53-dependent G1 checkpoint abnormalities, they are dependent on the G2 checkpoint. G2 checkpoint abrogation may therefore sensitize p53 deficient tumor cells to anti-cancer agents.
Reference:
1. Leijen S, el at., Curr Clin Pharmacol. 2010 Apr 21. [Epub ahead of print] PubMed PMID: 20406171.
2. Hirai H, et al., Cancer Biol Ther. 2010 Apr 4;9 (7). [Epub ahead of print] PubMed PMID: 20107315.
3. Hirai H, et al., Mol Cancer Ther. 2009 Nov; 8(11):2992-3000.
4: Mizuarai S, et al., Mol Cancer. 2009 Jun 8; 8:34. PubMed PMID: 19500427; PubMed Central PMCID: PMC2700070.
APIM050198: MK-1775 (ADAVOSERTIB) (AZD1775)
CAS No.: 955365-80-7.
Molecular Formula: C27H32N8O2.
Molecular Weight: 500.6 (refer to Certificate of Analysis, batch-specific).
Purity: >99.5% (HPLC).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0 °C (short term), -20 °C (long term), desiccated.
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