Chemical Properties | Back Directory | [Boiling point ]
766.7±70.0 °C(Predicted) | [density ]
1.311±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
12.91±0.20(Predicted) | [color ]
Light yellow to yellow |
Hazard Information | Back Directory | [Uses]
Azenosertib (ZN-c3) is a selective, orally active inhibitor for Wee1 inhibitor (IC50=3.9 nM). Azenosertib exhibits antitumor activity[1]. | [in vivo]
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]. Animal Model: | A427 xenograft NOD/SCID mice model[1] | Dosage: | 80 mg/kg | Administration: | p.o. for 28 days | Result: | Inhibited tumor growth. |
| [References]
[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. DOI:10.1021/acs.jmedchem.1c01121 |
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