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Targapremir-210

CAS No. 1049722-30-6

Targapremir-210( —— )

Catalog No. M33508 CAS No. 1049722-30-6

Targapremir-210 (TGP-210) is a selective and potent inhibitor of miRNA-210 (miRNA-210), which inhibits pre-miR-210 processing and induces apoptosis in breast cancer cells.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Targapremir-210
  • Note
    Research use only, not for human use.
  • Brief Description
    Targapremir-210 (TGP-210) is a selective and potent inhibitor of miRNA-210 (miRNA-210), which inhibits pre-miR-210 processing and induces apoptosis in breast cancer cells.
  • Description
    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.
  • In Vitro
    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.
  • In Vivo
    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.
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    Apoptosis
  • Recptor
    Apoptosis
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1049722-30-6
  • Formula Weight
    592.69
  • Molecular Formula
    C32H36N10O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (421.81 mM; Ultrasonic )
  • SMILES
    CN1CCN(CC1)c1ccc2nc([nH]c2c1)-c1ccc2nc([nH]c2c1)-c1cccc(OCCCC(=O)NCCCN=[N+]=[N-])c1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Costales MG, et al. Small Molecule Inhibition of microRNA-210 Reprograms an Oncogenic Hypoxic Circuit. J Am Chem Soc. 2017 Mar 8; 139(9):3446-3455.?
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