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产品价格:电议      采购度:1598      原产地:美洲
发布时间:2021/12/1 9:21:37 所属地区:国外 国外
简要描述:
Targaprimir-96 TFA 是 microRNA-96 (miR-96) 加工的有效抑制剂。Targaprimir-96 TFA 选择性地调节癌细胞中 miR-96 的产生并触发凋亡 (apoptosis)。Targaprimir-96 TFA 高亲和力的与 primary miR-96 (pri-miR-96) 结合。Targaprimir-96 TFA 直接与乳腺癌细胞中的 pri-
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CAS No. :
MCE 站:Targaprimir-96 TFA
产品活性:Targaprimir-96 TFA 是 microRNA-96 (miR-96) 加工的有效抑制剂。Targaprimir-96 TFA 选择性地调节癌细胞中 miR-96 的产生并触发凋亡 (apoptosis)。Targaprimir-96 TFA 高亲和力的与 primary miR-96 (pri-miR-96) 结合。Targaprimir-96 TFA 直接与乳腺癌细胞中的 pri-miR-96 结合,并不影响健康乳腺细胞。
研究领域:Epigenetics | Apoptosis
In Vitro: Targaprimir-96 TFA 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) TFA 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 TFA (50 nM; 48 hours) increases FOXO1 levels and triggers apoptosis in breast cancer cell line 4175.
Targaprimir-96 TFA 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 TFA 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.
In Vivo: Targaprimir-96 TFA (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 TFA 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.
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更新时间:2024/1/2 10:19:40
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