| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
The specific target of L2H2-6OTD formic is not provided in the available data. The related compound L2H2-6OTD acetate is a telomerase inhibitor analog that contains one to four G-quadruplex binding loops. It exhibits telomerase inhibitory activity with an IC₅0 of 15 nM by stabilizing G-quadruplex structures in the telomere DNA.
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| ln Vitro |
L2H2-6OTD formic is a specialized chelator designed for metal ion binding. The related compound L2H2-6OTD acetate contains one to four G-quadruplex binding loops and is a telomerase inhibitor analog. L2H2-6OTD acetate exhibits telomerase inhibitory activity with an IC₅0 value of 15 nM. The formic acid salt form (L2H2-6OTD formic) is expected to have similar telomerase inhibitory activity.
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| Enzyme Assay |
A general cell-free protocol for assessing G-quadruplex stabilization: A fluorescence resonance energy transfer (FRET) melting assay is used. A 5′-fluorescein-labeled and 3′-TAMRA-labeled oligonucleotide that forms a G-quadruplex structure (e.g., the human telomeric sequence d[AGGG(TTAGGG)3]) is used. The oligonucleotide (200 nM) is incubated in a buffer containing 100 mM KCl and 10 mM Tris-HCl (pH 7.4) with various concentrations of L2H2-6OTD formic or L2H2-6OTD acetate (0.1 nM to 100 uM). The samples are heated from 25degC to 95degC at a rate of 1degC per minute, and the fluorescence emission at 520 nm (FAM) is monitored. The melting temperature (Tm) of the G-quadruplex is determined. An increase in Tm indicates stabilization of the G-quadruplex by the compound. The deltaTm is calculated.
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| Cell Assay |
A general cellular protocol for assessing telomerase inhibition: A telomeric repeat amplification protocol (TRAP) assay is used to measure telomerase activity in cell lysates. Cells (e.g., HeLa, A549, or cancer cells with high telomerase activity) are treated with various concentrations of L2H2-6OTD formic (0.1 nM to 10 uM) for 48 hours. Cells are harvested, washed with PBS, and lysed in CHAPS lysis buffer on ice for 30 minutes. The lysates are centrifuged, and the supernatant is collected. Telomerase activity is measured using a TRAP assay kit. The cell lysate is incubated with a telomerase substrate primer (TS) and nucleotides at 30degC for 30 minutes, allowing telomerase to add telomeric repeats to the TS primer. The reaction mixture is then subjected to PCR amplification using the TS primer and a reverse primer (RP). The PCR products are separated by polyacrylamide gel electrophoresis and visualized by silver staining or SYBR Green. The intensity of the telomerase ladder is quantitated. The IC₅0 for telomerase inhibition is calculated.
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| Animal Protocol |
A general animal protocol for evaluating telomerase inhibitors in a xenograft model: Female BALB/c nude mice are subcutaneously injected with 5×10⁶ HeLa or other telomerase-positive cancer cells in 0.1 mL of PBS mixed with Matrigel (1:1). When the average tumor volume reaches 100-150 mm3, the mice are randomized into treatment groups (n=8-10 per group). L2H2-6OTD formic is formulated in a suitable vehicle (e.g., 10% DMSO, 40% PEG300, 5% Tween-80, 45% saline) and administered via intraperitoneal (IP) injection at doses of 5, 10, and 20 mg/kg once daily for 21 days. Tumor volume is measured twice weekly using a caliper, and body weight is recorded. At the end of the study, the mice are euthanized, and tumors are excised and weighed. Telomerase activity is measured in tumor lysates using the TRAP assay. Tumor tissues are also processed for immunohistochemistry (Ki-67 and cleaved caspase-3) and for assessment of telomere length by Southern blot or quantitative FISH (Q-FISH).
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| ADME/Pharmacokinetics |
General pharmacokinetic protocol for L2H2-6OTD formic: Male Sprague-Dawley rats are administered L2H2-6OTD formic via intraperitoneal (IP, 10 mg/kg) and intravenous (IV, 2 mg/kg) injection. The compound is formulated in a vehicle such as 10% DMSO, 40% PEG300, 5% Tween-80, 45% saline. Blood samples are collected at 0.083, 0.25, 0.5, 1, 2, 4, 8, 12, and 24 hours post-dose. Plasma concentrations of L2H2-6OTD formic are quantified by LC-MS/MS. PK parameters (Cmax, Tmax, AUC, t½, clearance, Vd, and IP bioavailability) are calculated using non-compartmental analysis.
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| Toxicity/Toxicokinetics |
General toxicity protocol for L2H2-6OTD formic: A 14-day repeated-dose toxicity study is performed in ICR mice. L2H2-6OTD formic is administered via intraperitoneal (IP) injection at doses of 5, 15, and 40 mg/kg/day for 14 consecutive days. Clinical signs, body weight, and food consumption are monitored daily. At the end of the study, blood samples are collected for hematology (complete blood count with differential) and serum chemistry (ALT, AST, ALP, BUN, creatinine, total protein, albumin, glucose). Gross necropsy is performed, and the weights of major organs (liver, kidney, spleen, heart, lung, brain, testes) are recorded. Histopathological examination of these organs is conducted. Bone marrow smears are prepared to assess any effects on hematopoietic cells. Due to the role of telomerase in stem cells, careful monitoring of hematopoietic and gastrointestinal systems is recommended.
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| References | |
| Additional Infomation |
L2H2-6OTD formic has a molecular formula of C31H32N10O10 and a molecular weight of 704.65. The compound appears as a solid powder with a purity of ≥98%. It does not have a CAS number listed. L2H2-6OTD formic is a specialized chelator designed for metal ion binding in biochemical and medicinal chemistry research. It is involved in metal homeostasis, neurodegenerative diseases, and cancer therapies. The compound is also known as L2H2-6OTD acetate. It is a valuable tool for studying telomerase inhibition, G-quadruplex stabilization, and their effects on cancer cell growth.
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| Molecular Formula |
C31H32N10O10
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| Molecular Weight |
704.65
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| Appearance |
Solid powder
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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 (e.g. under nitrogen), 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) |
H2O : ≥ 100 mg/mL (141.91 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 | 1.4191 mL | 7.0957 mL | 14.1914 mL | |
| 5 mM | 0.2838 mL | 1.4191 mL | 2.8383 mL | |
| 10 mM | 0.1419 mL | 0.7096 mL | 1.4191 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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