2093449-12-6
Chemical Structure
ASTX295
- CAS No.: 2093449-12-6
- Formula:C33H34Cl2FNO6
- Molecular Weight:630.53
InChIKey: JDCHPEZNOKLHPK-KJEAJVGRSA-N
SMILES: CO[C@](C(C(C1=O)=C2)=C(F)C=C2[C@@](CC)(O)C3CCOCC3)(N1[C@H](C4=CC=C(Cl)C=C4)[C@H](C)C(O)=O)C5=CC=C(Cl)C=C5
Biological Activity: ASTX295 is an orally active and selective MDM2 antagonist with an IC50 of <1 nM. ASTX295 inhibits the MDM2-p53 interaction, activates wild-type TP53, and thereby induces the expression of relevant transcriptional targets, leading to cell death. ASTX295 drives the transition of pancreatic cancer cells from senescence to apoptosis and regulates p53 and DNA damage biomarkers. ASTX295 can be used for the research of hematologic malignancies and pancreatic cancer[1][2].
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ASTX295 | 99.81% | ASTX295 is an orally active and selective MDM2 antagonist with an IC50 of <1 nM. ASTX295 inhibits the MDM2-p53 interaction, activates wild-type TP53, and thereby induces the expression of relevant transcriptional targets, leading to cell death. ASTX295 drives the transition of pancreatic cancer cells from senescence to apoptosis and regulates p53 and DNA damage biomarkers. ASTX295 can be used for the research of hematologic malignancies and pancreatic cancer. | ||||||||||||||||||||
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- [1]. Iqbal N, et al. ASTX295 a Novel Potent MDM2 Antagonist Induces More Than One Mechanism of Programmed Cell Death (PCD) in Lymphoid Malignancies[J]. Blood, 2024, 144: 3591.
- [2]. Ward G, et al. Switching cell fate from senescence to apoptosis by the combination of a p53 corrector with the MDM2 antagonist ASTX295[C]//Cancer Research. 615 CHESTNUT ST, 17TH FLOOR, PHILADELPHIA, PA 19106-4404 USA: AMER ASSOC CANCER RESEARCH, 2025, 85(8).
Keywords
