| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The intermediate itself has no direct biological target. L2H2-6OTD, the compound for which this intermediate is used, targets the telomerase enzyme, which is responsible for maintaining telomere length in cancer cells. Telomerase is a reverse transcriptase that adds DNA sequence repeats to chromosome ends.
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| ln Vitro |
L2H2-6OTD intermediate-1 has no direct in vitro biological activity. The final compound L2H2-6OTD exhibits potent in vitro telomerase inhibitory activity with an IC50 of 15 nM, making it a highly potent telomerase inhibitor. It is a synthetic analogue of the natural product telomestatin.
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| ln Vivo |
The intermediate itself has no direct in vivo activity. L2H2-6OTD has been shown to inhibit telomerase activity in cells, leading to progressive telomere shortening and eventual growth arrest or apoptosis in telomerase-expressing cancer cells. However, detailed in vivo xenograft data for L2H2-6OTD is limited.
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| Enzyme Assay |
As a chemical intermediate, L2H2-6OTD intermediate-1 is not used in biological enzyme assays. For quality control, standard chemical analysis includes HPLC for purity assessment (typically 98% or higher), LC-MS for molecular weight confirmation (520.6 g/mol), and NMR for structural verification.
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| Cell Assay |
Cell-based assays are not performed directly on this intermediate. For L2H2-6OTD, typical protocols involve seeding telomerase-positive cancer cells (e.g., HeLa, HCT-116) in culture, treating with 1-100 nM of the compound for 3-7 days, and measuring telomerase activity by TRAP assay (telomeric repeat amplification protocol).
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| Animal Protocol |
Animal studies are not conducted on this intermediate. For L2H2-6OTD, typical xenograft protocols would involve subcutaneous implantation of human cancer cells into immunocompromised mice, followed by compound administration (e.g., intraperitoneal injection at 1-10 mg/kg) and monitoring of tumor growth, telomere length, and survival.
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| ADME/Pharmacokinetics |
No pharmacokinetic data is available for this intermediate. For L2H2-6OTD, PK studies would be essential for evaluating its potential as a therapeutic, but such data is not publicly available. Researchers may need to conduct their own PK assessments in relevant models.
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| Toxicity/Toxicokinetics |
No direct toxicity data is available for this intermediate. For L2H2-6OTD, as a telomerase inhibitor, its toxicity profile would be related to the delayed effects of telomere shortening on rapidly dividing cell populations. Standard safety precautions should be taken when handling this research chemical.
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| References |
[1]. Doi Takayuki, et al. Total Synthesis of (R)-Telomestatin. Organic Letters (2006), 8(18), 4165-4167.
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| Additional Infomation |
L2H2-6OTD intermediate-1 is a research-use chemical and not a pharmaceutical for human consumption. L2H2-6OTD is a synthetic macrocyclic heptaoxazole analog of telomestatin, a natural product known to stabilize G-quadruplex structures in telomeric DNA, thereby inhibiting telomerase. This compound is not approved for clinical use and is for research purposes only.
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| Exact Mass |
520.199
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|---|---|
| CAS # |
912656-47-4
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| PubChem CID |
11954833
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
36
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| Complexity |
775
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=C(N=C(O1)C2=C(OC(=N2)[C@H](CSC(C)(C)C)NC(=O)OC(C)(C)C)C)C3=NC(=CO3)C(=O)OC
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| InChi Key |
FFQDCASBDSSMOP-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C24H32N4O7S/c1-12-16(19-25-14(10-32-19)21(29)31-9)28-20(34-12)17-13(2)33-18(27-17)15(11-36-24(6,7)8)26-22(30)35-23(3,4)5/h10,15H,11H2,1-9H3,(H,26,30)/t15-/m0/s1
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| Chemical Name |
methyl 2-[2-[2-[(1R)-2-tert-butylsulfanyl-1-[(2-methylpropan-2-yl)oxycarbonylamino]ethyl]-5-methyl-1,3-oxazol-4-yl]-5-methyl-1,3-oxazol-4-yl]-1,3-oxazole-4-carboxylate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
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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