Azenosertib

• CAT Number: I038761
• CAS Number: 2376146-48-2
• Molecular Formula: C29H34N8O2
• Molecular Weight: 526.63
• Purity: ≥95%
• Synonyms: 1-[(7R)-7-ethyl-7-hydroxy-5,6-dihydrocyclopenta[b]pyridin-2-yl]-6-[4-(4-methylpiperazin-1-yl)anilino]-2-prop-2-enylpyrazolo[3,4-d]pyrimidin-3-one
• InChI: InChI=1S/C29H34N8O2/c1-4-14-36-27(38)23-19-30-28(31-21-7-9-22(10-8-21)35-17-15-34(3)16-18-35)33-26(23)37(36)24-11-6-20-12-13-29(39,5-2)25(20)32-24/h4,6-11,19,39H,1,5,12-18H2,2-3H3,(H,30,31,33)/t29-/m1/s1
• InChIKey: OXTSYWDBUVRXFF-GDLZYMKVSA-N
• SMILES: CCC1(CCC2=C1N=C(C=C2)N3C4=NC(=NC=C4C(=O)N3CC=C)NC5=CC=C(C=C5)N6CCN(CC6)C)O

Azenosertib (Cat No.: I038761) is an investigational small-molecule inhibitor of WEE1, a kinase that regulates the G2/M cell cycle checkpoint by inhibiting CDK1 activity. By blocking WEE1, azenosertib forces cancer cells with DNA damage to prematurely enter mitosis, leading to mitotic catastrophe and cell death. This mechanism is especially effective in tumors with p53 deficiencies. Azenosertib is being evaluated in clinical trials for solid tumors and hematologic malignancies and shows promise as a monotherapy or in combination regimens.

Reference

[1]. Huang PQ, et al. Discovery of ZN-c3, a Highly Potent and Selective Wee1 Inhibitor Undergoing Evaluation in Clinical Trials for the Treatment of Cancer [published online ahead of print, 2021 Aug 23]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01121.
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