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Purity: ≥98%
Targapremir-210 (TGP-210) is a novel potent and selective inhibitor of microRNA-210 with anticancer activity. Targapremir-210 inhibits tumorigenesis in a mouse xenograft model of hypoxic triple negative breast cancer. Targapremir-210 selectively recognizes the miR-210 precursor and can differentially recognize RNAs in cells that have the same target motif but have different expression levels, revealing this important feature for selectively drugging RNAs for the first time. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM).
| ln Vitro |
In MDA-MB-231 cells grown under hypoxic conditions, targapremir-210 decreases the amount of mature miR-210 with an IC50 of approximately 200 nM [1]. MDA-MB-231 cells are specifically induced to undergo apoptosis in hypoxic environments by tigapremir-210 (200 nM). When MDA-MB-231 cells are cultivated in normoxic conditions, tartapremir-210 does not cause apoptosis, but it does when the conditions are hypoxic [1].
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| ln Vivo |
Targapremir-210 (100 μL, 200 nM; intraperitoneal injection once) inhibits triple-negative breast cancer (TNBC) cell growth in MDA-MB-231 in vivo. In TNBC animal models, tartapremir-210 decreases tumor burden and can bind to tumors for up to 21 days [1].
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| Animal Protocol |
Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse were subcutaneously (sc) (sc) transplanted with cell suspension into the breast fat pad [1].
Doses: 100 μL, 200 nM Route of Administration: Single intraperitoneal (ip) injection 24 hrs (hrs (hours)) after transplantation Experimental Results: diminished tumor growth as assessed by luciferase signal intensity and quality of resected tumors. |
| 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.
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| Molecular Formula |
C32H36N10O2
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|---|---|
| Molecular Weight |
592.694045066834
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| CAS # |
1049722-30-6
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| SMILES |
O=C(NCCCN=[N+]=[N-])CCCOC1=CC=CC(C2=NC3=CC=C(C4=NC5=CC=C(N6CCN(C)CC6)C=C5N4)C=C3N2)=C1
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| InChi Key |
PAYVJEWMAWLKAP-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
N-(3-Azidopropyl)-4-[3-[6-(4-methyl-1-piperazinyl)[2,6'-bi-1H-benzimidazol]-2'-yl]phenoxy]-butanamide
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| Synonyms |
TGP-210Targapremir-210 TGP 210Targapremir 210 TGP210 Targapremir210
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~421.81 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6872 mL | 8.4361 mL | 16.8722 mL | |
| 5 mM | 0.3374 mL | 1.6872 mL | 3.3744 mL | |
| 10 mM | 0.1687 mL | 0.8436 mL | 1.6872 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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