| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| 25mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Namitecan targets topoisomerase I, an enzyme that relieves torsional stress in DNA during replication and transcription. By stabilizing the topoisomerase I-DNA cleavage complex, it prevents the relegation of the DNA strand, leading to the accumulation of DNA breaks and ultimately cell death. This mechanism is characteristic of the camptothecin class of topoisomerase I inhibitors.
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| ln Vitro |
Cetuximab and namitecan work together to suppress EGFR expression. In various cell lines, namitecan causes an EGFR expression reduction that is dose-dependent [1]. A431 and A431/TPT cells undergo similar degrees of apoptosis when exposed to ST1968, with IC50 values of 0.21 and 0.29 μM, respectively [2].
In vitro, Namitecan is a potent topoisomerase I inhibitor. It induces a dose-dependent decrease in EGFR expression in various cell lines. It induces a comparable level of apoptosis in A431 and A431/TPT cells with IC50 values of 0.21 and 0.29 μM, respectively. Its potent antitumor activity makes it a valuable research compound. |
| ln Vivo |
In SCC models, a combination of cetuximab (1 mg/mouse) and napitecan (10 mg/kg) causes synergistic antitumor effects based on the copy number of the EGFR gene [1]. There were no hazardous deaths and a tolerable weight loss with ST1968 (25 mg/kg). In mice bearing A431 tumors, ST1968 elicited a 100% complete response rate and continued to exhibit meaningful activity in tumors resistant to topotecan [2].
In vivo, Namitecan has shown antitumor activity in preclinical models. As a water-soluble camptothecin analog, it may offer advantages in terms of formulation and administration compared to other camptothecins. Its ability to inhibit topoisomerase I and induce apoptosis translates to tumor growth inhibition in vivo. |
| Enzyme Assay |
The in vitro activity of Namitecan against topoisomerase I is determined using cell-free assays. In a typical protocol, the topoisomerase I enzyme is incubated with a DNA substrate and varying concentrations of Namitecan. The formation of the cleavage complex is measured, and the IC50 is calculated. This assay directly measures the compound's ability to inhibit the enzyme.
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| Cell Assay |
Cellular assays for Namitecan involve studying its effect on cell viability and apoptosis. In a typical protocol, cancer cells (e.g., A431) are treated with increasing concentrations of Namitecan. Cell viability is measured using an MTT or CellTiter-Glo assay. Apoptosis is quantified by measuring caspase activity or by staining with Annexin V and propidium iodide. The IC50 for cell growth inhibition is determined.
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| Animal Protocol |
The in vivo efficacy of Namitecan is evaluated in xenograft mouse models. In these studies, human tumor cells are implanted subcutaneously into immunodeficient mice. When tumors reach a certain size, the animals are treated with Namitecan, typically via intravenous injection. Tumor growth is monitored by caliper measurements, and tumor weights are assessed at the end of the study.
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| ADME/Pharmacokinetics |
Namitecan is a water-soluble camptothecin analog. It has a molecular weight of 423.42 and a molecular formula of C₂₂H₂₁N₃O₆. As a topoisomerase I inhibitor, it is a member of the camptothecin class of anticancer agents. Its water solubility is a key feature that may facilitate its formulation and administration.
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| Toxicity/Toxicokinetics |
The toxicity of Namitecan is related to its mechanism of action as a topoisomerase I inhibitor. Like other camptothecins, its primary dose-limiting toxicity is expected to be myelosuppression and gastrointestinal toxicity. Its safety profile would be carefully evaluated in preclinical and clinical studies.
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| References |
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| Additional Infomation |
Namitecan has been used in trials investigating the treatment of solid tumors.
Namitecan (ST-1968) is a novel, potent, and water-soluble camptothecin analog that acts as a topoisomerase I inhibitor. It has high antitumor activity and induces apoptosis in cancer cells. It is a research compound being investigated for its potential as an anticancer agent, but it is not an approved drug. |
| Molecular Formula |
C23H22N4O5
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|---|---|
| Molecular Weight |
434.452
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| Exact Mass |
434.159
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| CAS # |
372105-27-6
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| Related CAS # |
372105-27-6;
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| PubChem CID |
10950142
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.089
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
899
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C(C5=CC=CC=C5N=C4C3=C2)/C=N/OCCN)O
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| InChi Key |
IBTISPLPBBHVSU-UVOOVGFISA-N
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| InChi Code |
InChI=1S/C23H22N4O5/c1-2-23(30)17-9-19-20-15(11-27(19)21(28)16(17)12-31-22(23)29)14(10-25-32-8-7-24)13-5-3-4-6-18(13)26-20/h3-6,9-10,30H,2,7-8,11-12,24H2,1H3/b25-10+/t23-/m0/s1
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| Chemical Name |
(4S)-11-((E)-((2-Aminoethoxy)imino)methyl)-4-ethyl-4-hydroxy-1,12-dihydro-14H-pyrano(3',4'
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| Synonyms |
ST-1968 ST 1968 ST1968
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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 (~575.45 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.79 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 (4.79 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 | 2.3018 mL | 11.5088 mL | 23.0176 mL | |
| 5 mM | 0.4604 mL | 2.3018 mL | 4.6035 mL | |
| 10 mM | 0.2302 mL | 1.1509 mL | 2.3018 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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