Targaprimir-96 TFA

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Targaprimir-96 TFA 

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。

Targaprimir-96 TFA

Targaprimir-96 TFA Chemical Structure

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生物活性

Targaprimir-96 TFA is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 TFA selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 TFA binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 TFA directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells[1].

体外研究
(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[1].
Targaprimir-96 TFA (50 nM; 48 hours) increases FOXO1 levels and triggers apoptosis in breast cancer cell line 4175[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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)[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 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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

1505.77

Formula

C79H103F3N18O9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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