Identification | Back Directory | [Name]
Targaprimir-96 | [CAS]
1655508-14-7 | [Synonyms]
Targaprimir-96 Glycinamide, N-[4-[3-[6-(4-methyl-1-piperazinyl)[2,6'-bi-1H-benzimidazol]-2'-yl]phenoxy]-1-oxobutyl]-N-propylglycyl-N-propylglycyl-N2-[[1-[3-[[4-[2,6-bis(1,1-dimethylethyl)-4-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]phenoxy]-1-oxobutyl]amino]propyl]-1H-1,2,3-triazol-4-yl]methyl]- | [Molecular Formula]
C77H102N18O7 | [MDL Number]
MFCD34469749 | [MOL File]
1655508-14-7.mol | [Molecular Weight]
1391.75 |
Hazard Information | Back Directory | [Uses]
Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells[1]. | [in vivo]
Targaprimir-96 (10 mg/kg; i.p.; every other day for 21 days) inhibits tumor growth in a mouse model of triple-negative breast cancer (TNBC)[1].
The amount of Targaprimir-96 (2 or 7 mg/kg; i.p.) in plasma peaks is ~4 h in FVB/n mice. Importantly, even 48 hours postinjection, the concentration of Targaprimir-96 remaining in plasma is much greater than the 50 nM cellular concentration that triggered apoptosis: 1.6 μM for the 2 mg/kg dosage and 1.9 μM for the 7 mg/kg dosage[1]. Animal Model: | Female NOD/Scid mice (Mouse Model of TNBC)[1] | Dosage: | 10 mg/kg | Administration: | i.p.; every other day for 21 days | Result: | Decreased levels of mature miR-96 by ~50% and increased levels of pri-miR-96, with a concomitant increase of FOXO1. No toxicity was observed. |
| [References]
[1] Velagapudi SP, et al. Design of a small molecule against an oncogenic noncoding RNA. Proc Natl Acad Sci U S A. 2016 May 24;113(21):5898-903. DOI:10.1073/pnas.1523975113 |
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