| Bioactivity | AGX51 is a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits the TNBC cell lines with IC50s of nearly 25 μM. AGX51 can be used for the research of cancer[1]. | ||||||||||||
| Target | IC50: 26.66 μM (4T1), 8.7 μM (HMLE RAS Twist), 22.28 μM (MDA-MB-157), 30.91 μM (MDA-MB-436), 36.55 μM (SK-BR-3), 60 μM (MCF-7), 10.89 μM (PDX-BR7), 11.97 μM (PDX-IBT) , 18.56 μM (PDX-BR11) | ||||||||||||
| Invitro | AGX51 (0-80 μM; 24 h) decreases ID1 protein levels in 4T1 cells[1].AGX51 (40 μM; 0-72 h) decreases ID1 levels protein with a 40 μM concentratio in 4T1 cells[1].AGX51 (40 μM; 24 h) influences 4T1 cells , ER+, HER2+, TNBC and three breast cancer PDX cell ines[1].AGX51 (0-80 μM; 24-48 h) influences cell cycle of 4T1 cells[1].AGX51 (40 μM; 4-24 h) influences phospho-histone H3 levels in 4T1 cells[1].AGX51 (40 μM; 24 h) influences ROS levels in 4T1 cells[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| In Vivo | AGX51 (50 mg/kg; i.p. twice a day for 4 weeks) inhibits lung metastasis[1].AGX51 (15 mg/kg; i.p. twice a day for 3 weeks) exibits anti-tumor activity with autochronous cancer[1]. Animal Model: | ||||||||||||
| Name | AGX51 | ||||||||||||
| CAS | 330834-54-3 | ||||||||||||
| Formula | C27H29NO4 | ||||||||||||
| Molar Mass | 431.52 | ||||||||||||
| Appearance | Oil | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Wojnarowicz PM, et al. Anti-tumor effects of an ID antagonist with no observed acquired resistance. NPJ Breast Cancer. 2021 May 24;7(1):58. |