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编 号：F198941
分子式：C77H102N18O7
分子量：1391.75
分子式：C77H102N18O7
分子量：1391.75
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CAS No: 1655508-14-7
产品详情
生物活性：
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.
体内研究：
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).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.Animal Model:Female NOD/Scid mice (Mouse Model of TNBC)
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.
体外研究：
Targaprimir-96 shows a dose-response in MDA-MB-231 triple negative breast cancer cells with an IC50 of ~50 nM by assessing the reduction of mature miR-96 levels. Targaprimir-96 (50 nM) boosts the amount of the pri-miRNA and decreases the levels of the pre-miRNA and mature miRNA in a dose-dependent manner.Targaprimir-96 (50 nM; 48 hours) increases FOXO1 levels and triggers apoptosis in breast cancer cell line 4175.Targaprimir-96 binds RNA3 (contains both the Drosha site and the adjacent 1×1 nt GG internal loop) with a Kd of 85 nM. Targaprimir-96 binds RNA1, RNA2, RNA4, and RNA5 with Kd values of 1.2, 0.9, 1.2, and 1.5 μM, respectively. Thus, Targaprimir-96 is highly RNA-selective and recognizes both the 1×1 nt GG and 1×1 nt UU loops to provide high affinity, effectively discriminating against a variety of related targets.
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.
体内研究：
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).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.Animal Model:Female NOD/Scid mice (Mouse Model of TNBC)
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.
体外研究：
Targaprimir-96 shows a dose-response in MDA-MB-231 triple negative breast cancer cells with an IC50 of ~50 nM by assessing the reduction of mature miR-96 levels. Targaprimir-96 (50 nM) boosts the amount of the pri-miRNA and decreases the levels of the pre-miRNA and mature miRNA in a dose-dependent manner.Targaprimir-96 (50 nM; 48 hours) increases FOXO1 levels and triggers apoptosis in breast cancer cell line 4175.Targaprimir-96 binds RNA3 (contains both the Drosha site and the adjacent 1×1 nt GG internal loop) with a Kd of 85 nM. Targaprimir-96 binds RNA1, RNA2, RNA4, and RNA5 with Kd values of 1.2, 0.9, 1.2, and 1.5 μM, respectively. Thus, Targaprimir-96 is highly RNA-selective and recognizes both the 1×1 nt GG and 1×1 nt UU loops to provide high affinity, effectively discriminating against a variety of related targets.
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