| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
G-quadruplex (G4) DNA structures and telomerase.
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| ln Vitro |
360A iodide inhibits telomerase activity and stabilizes G-quadruplexes with an IC50 of 300 nM for telomerase in the TRAP-G4 test. 360A lowers the viability of glioma cell lines (such as T98G, CB193, U118-MG, SAOS-2 and primary astrocytes) with IC50 of 4.8 ± 1.1 μM, 3.9 ± 0.4 μM, 8.4 ± 0.5 μM, > 15 μM and 17.4 ±1.2 μM respectively[1]. 360A generates Rad51-dependent telomere abnormalities that primarily affect lagging strand telomeres, including telomere loss or telomeric doublets, and induces DNA-PKcs-dependent sister-telomere fusion [2].
In vitro, 360A iodide binds to G-quadruplex structures with strong affinity and selectivity, stabilizing these non-canonical DNA conformations. It inhibits telomerase activity with an IC₅0 of 300 nM in TRAP-G4 assays. The compound lowers the viability of glioma cell lines with varying potencies: IC₅0 values are 4.8+/-1.1 microM (T98G), 3.9+/-0.4 microM (CB193), 8.4+/-0.5 microM (U118-MG), >15 microM (SAOS-2), and 17.4+/-1.2 microM (primary astrocytes). G-quadruplex stabilization by 360A can interfere with telomerase access to telomeric DNA, disrupt gene expression, and inhibit DNA replication. |
| ln Vivo |
360A iodide is a research compound used primarily in cell-based and biochemical assays; no specific in vivo efficacy data are reported. As a G-quadruplex stabilizer, it has potential applications in cancer research, but in vivo studies are limited. The compound may be used in xenograft models to evaluate anti-tumor activity, though such studies are not described in the available literature.
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| Enzyme Assay |
G-quadruplex binding and stabilization are assessed using biophysical methods. Fluorescence resonance energy transfer (FRET) melting assays are performed using fluorescently labeled G-quadruplex-forming oligonucleotides. The oligonucleotide (0.2-0.5 microM) is incubated with 360A iodide at various concentrations (0.01-10 microM) in buffer containing 10 mM Tris-HCl (pH 7.4) and 100 mM KCl. Fluorescence is measured at increasing temperatures (25-95degC) to determine the melting temperature (Tm) of the G-quadruplex. An increase in Tm indicates stabilization. Surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) can be used to measure binding affinity and thermodynamics. Telomerase activity is measured using the TRAP-G4 assay. Cell viability is assessed using MTT or CellTiter-Glo assays in various cancer cell lines.
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| Cell Assay |
Cancer cell lines (e.g., T98G, CB193, U118-MG, SAOS-2) and primary astrocytes are cultured in appropriate medium. Cells are seeded in 96-well plates at 5,000-10,000 cells/well and allowed to adhere for 24 hours. 360A iodide is added at concentrations ranging from 0.1-50 microM and incubated for 48-72 hours. Cell viability is measured using MTT assay: MTT reagent is added, incubated for 2-4 hours, formazan crystals are dissolved in DMSO, and absorbance is read at 570 nm. IC₅0 values are calculated from dose-response curves. For telomerase activity assays, cells are treated with the compound for 24-48 hours, cell lysates are prepared, and telomerase activity is measured using TRAP (telomeric repeat amplification protocol) assays with or without G-quadruplex stabilization conditions.
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| Animal Protocol |
360A iodide may be evaluated in mouse xenograft models for anti-tumor efficacy. Immunodeficient mice are implanted subcutaneously with tumor cells (e.g., glioma cell lines). When tumors reach a certain size, 360A iodide is administered intraperitoneally or orally at doses determined from preliminary studies (typically 10-50 mg/kg). Tumor volume is measured every 2-3 days using calipers. Body weight and general health are monitored. At study termination, tumors are excised for histological and molecular analysis (e.g., G-quadruplex stabilization, telomerase activity, apoptosis markers). However, detailed in vivo protocols are not described in publicly available literature for this specific compound.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 360A iodide (C2₇H23I2N₅O2) are not extensively reported. As a small-molecule G-quadruplex ligand, it is expected to have moderate lipophilicity and cellular permeability. The iodide salt form is used to enhance solubility. Metabolism and elimination pathways are not characterized in the available literature. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for 360A iodide. As a DNA-interacting compound, it may have genotoxic potential and should be handled with appropriate precautions. The compound is for research use only and not for human therapeutic use. Standard safety precautions for handling DNA-interactive compounds should be observed.
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| References |
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| Additional Infomation |
360A iodide is a G-quadruplex stabilizer and telomerase inhibitor used in cancer and genomic research. It is a 2,6-pyridine-dicarboxamide derivative with strong affinity and selectivity for G-quadruplex structures. The compound has been studied for its effects on glioma cell lines, showing selective cytotoxicity. 360A iodide is not an approved therapeutic agent; it is a research tool for studying G-quadruplex biology and telomerase inhibition. The iodide salt form (CAS 737763-37-0) is used for research applications.
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| Molecular Formula |
C27H23N5O2+2.2[I-]
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|---|---|
| Molecular Weight |
703.312
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| Exact Mass |
702.994
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| CAS # |
737763-37-0
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| Related CAS # |
360A;794458-56-3
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| PubChem CID |
78357792
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
36
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| Complexity |
674
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1=CC(C=CC=C2)=C2[N+](C)=C1)C3=CC=CC(C(NC4=C[N+](C)=C(C=CC=C5)C5=C4)=O)=N3.[I-].[I-]
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| InChi Key |
CYDYPTJPHHNFEL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H21N5O2.2HI/c1-31-16-20(14-18-8-3-5-12-24(18)31)28-26(33)22-10-7-11-23(30-22)27(34)29-21-15-19-9-4-6-13-25(19)32(2)17-21;;/h3-17H,1-2H3;2*1H
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| Chemical Name |
2-N,6-N-bis(1-methylquinolin-1-ium-3-yl)pyridine-2,6-dicarboxamide;diiodide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~2 mg/mL (~2.84 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4218 mL | 7.1092 mL | 14.2185 mL | |
| 5 mM | 0.2844 mL | 1.4218 mL | 2.8437 mL | |
| 10 mM | 0.1422 mL | 0.7109 mL | 1.4218 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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