Targapremir-210


Catalog No. Size PriceQuantity
M12470-2 2mg solid $220
M12470-10 10mg solid $795

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).

Product information

CAS Number: 1049722-30-6

Molecular Weight: 592.69

Formula: C32H36N10O2

Synonym:

TGP-210

Chemical Name: N-(3-azidopropyl)-4-(3-{6-[6-(4-methylpiperazin-1-yl)-1H-1, 3-benzodiazol-2-yl]-1H-1, 3-benzodiazol-2-yl}phenoxy)butanamide

Smiles: CN1CCN(CC1)C1=CC2NC(=NC=2C=C1)C1=CC2NC(=NC=2C=C1)C1=CC(=CC=C1)OCCCC(=O)NCCCN=[N+]=[N-]

InChiKey: PAYVJEWMAWLKAP-UHFFFAOYSA-N

InChi: InChI=1S/C32H36N10O2/c1-41-14-16-42(17-15-41)24-9-11-27-29(21-24)39-32(37-27)23-8-10-26-28(20-23)38-31(36-26)22-5-2-6-25(19-22)44-18-3-7-30(43)34-12-4-13-35-40-33/h2,5-6,8-11,19-21H,3-4,7,12-18H2,1H3,(H,34,43)(H,36,38)(H,37,39)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 250 mg/mL (421.81 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

References:

  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.

Products are for research use only. Not for human use.

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