Targapremir-210

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Targapremir-210 (TGP-210) 是一种有效的、选择性的 miR-210 (miRNA-210, microRNA-210) 抑制剂。 Targapremir-210 以高亲和力抑制 pre-miR-210 的加工 (Kd~200 nM)。Targapremir-210 是一种点击化学试剂。它含有 Azide 基团，可以和含有 Alkyne 基团的分子发生铜催化的叠氮-炔环加成反应（CuAAc)。还可以和含有 DBCO 或 BCN 基团的分子发生菌株促进的炔-叠氮环加成反应 (SPAAC)。

Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM). Targapremir-210 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

Targapremir-210 decreases mature miR-210 levels in MDA-MB-231 cells cultured under hypoxic conditions, with an IC50 of ～200 nM.Targapremir-210 (200 nM) induces MDA-MB-231 cells apoptosis is selective for the hypoxic environment. Targapremir-210 induces cells apoptosis under hypoxic conditions and does not induce apoptosis in MDA-MB-231 cells cultured in normoxia.

Targapremir-210 (100 μL of 200 nM; single i.p. injection) impedes MDA-MB-231 triple negative breast cancer (TNBC) cells proliferation in vivo. Targapremir-210 is able to reach the tumor and sustain for the entire 21-day period, and decreases tumor burden in a TNBC mouse model.Animal Model:NOD/SCID mice were subcutaneously transplanted cell suspension into breast fat pads.Dosage:100 μL of 200 nM Administration:Single i.p. injection 24 h post-transplantation Result:Decreased tumor growth as assessed by luciferase signal intensity and mass of the resected tumor.

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Apoptosis

Apoptosis

Apoptosis

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1049722-30-6

592.69

C32H36N10O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (421.81 mM; 超声助溶 )

CN1CCN(CC1)c1ccc2nc([nH]c2c1)-c1ccc2nc([nH]c2c1)-c1cccc(OCCCC(=O)NCCCN=[N+]=[N-])c1

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(-20℃)

With Ice Pack

≥ 2 years