For research use only. Not for therapeutic Use.
Azenosertib (ZN-c3) is a selective, orally active inhibitor for Wee1 inhibitor (IC50=3.9 nM). Azenosertib exhibits antitumor activity[1].
Azenosertib inhibits proliferations of cancer cells H23 and A427 with IC50s 103 and 75 nM[1].
Azenosertib (80 mg/kg; p.o.; 28 days) inhibits tumor growth in A427 xenograft NOD/SCID mice model[1].
Azenosertib (10 mg/kg, p.o.) shows plasma exposure Cmax of 2.1 μM, a half-time T1/2 of 2.3 h, an AUC0-24 h of 9.7 μM·h, and an oralbioavailability of F=142% in beagle dog model[1].
| Catalog Number | I038761 |
| CAS Number | 2376146-48-2 |
| 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 |
| Molecular Formula | C29H34N8O2 |
| Purity | ≥95% |
| 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 |
| 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. |
