| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| 10mg | |||
| 25mg | |||
| 50mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Targapremir-210 targets microRNA-210 (miR-210). It binds to the Dicer site of the miR-210 hairpin precursor and inhibits Dicer processing of the miRNA. It inhibits pre-miR-210 processing.
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|---|---|
| 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].
In vitro, targapremir-210 inhibits miR-210 with an IC50 of 200 nM in MDA-MB-231 breast cancer cells. It induces apoptosis in breast cancer cells. It induces cell apoptosis under hypoxic conditions. |
| 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].
In vivo, targapremir-210 has shown potential in preclinical studies for its ability to inhibit tumor growth and enhance sensitivity to chemotherapy in various cancer models. It decreases tumor burden in a triple-negative breast cancer (TNBC) mouse model. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for targapremir-210 typically involve evaluating its binding affinity to the miR-210 hairpin precursor using surface plasmon resonance or fluorescence polarization. Kd values are determined by measuring binding to the Dicer site.
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| Cell Assay |
For in vitro cell-based assays, targapremir-210 is dissolved in DMSO and applied to cultured breast cancer cells at concentrations ranging from 10 nM to 10 µM. Effects on miR-210 levels, apoptosis, and cell viability are assessed after 24-72 hours of treatment.
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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. In vivo animal studies commonly use mouse xenograft models of triple-negative breast cancer. Targapremir-210 is administered intraperitoneally (100 µL of 200 nM; single i.p.). Efficacy is evaluated by measuring tumor volume, tumor weight, and apoptosis. |
| ADME/Pharmacokinetics |
Targapremir-210 is a selective and potent inhibitor of miR-210. It is soluble in DMSO. It is typically stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
Targapremir-210 has a favorable safety profile with no significant toxicity reported at therapeutic doses. Its selectivity for miR-210 minimizes off-target effects.
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| 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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| Additional Infomation |
Targapremir-210 is a novel potent and selective inhibitor of microRNA-210 with anticancer activity. It inhibits tumorigenesis in a mouse xenograft model of hypoxic triple-negative breast cancer. Its unique mechanism of action positions it as a promising therapeutic candidate for targeting miRNA-related pathways in cancer treatment.
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| Molecular Formula |
C32H36N10O2
|
|---|---|
| Molecular Weight |
592.694045066834
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| Exact Mass |
592.302
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| CAS # |
1049722-30-6
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| PubChem CID |
44221088
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.59
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
44
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| Complexity |
973
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O(CCCC(NCCCN=[N+]=[N-])=O)C1=CC=CC(=C1)C1=NC2=CC=C(C=C2N1)C1=NC2=CC=C(C=C2N1)N1CCN(C)CC1
|
| 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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| HS Tariff Code |
2934.99.9001
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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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