| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Topoisomerase I (Topo I); targets involved in DNA replication and cell division in cancer cells.
|
|---|---|
| ln Vitro |
In vitro, 7-Ethylcamptothecin exhibits strong cytotoxic activity against various murine tumors, including L1210 leukemia and Walker 256 carcinosarcoma. It shows anticancer activity against lung, breast, and colon cancer cell lines. As a Topo I inhibitor, it stabilizes the topoisomerase I-DNA cleavage complex, leading to DNA damage and apoptosis. However, quantitative IC50 values for specific cell lines are not detailed in publicly available sources.
|
| ln Vivo |
In vivo, 7-Ethylcamptothecin shows strong activity against various murine tumors, including L1210 leukemia and Walker 256 carcinosarcoma models. It is effective against drug-resistant tumors. Detailed dose-response and pharmacokinetic data in animal models are limited in publicly available literature.
|
| Enzyme Assay |
No specific cell-free Topo I assay protocol is detailed for 7-Ethylcamptothecin. For topoisomerase I inhibitors, typical cell-free assays involve incubating the compound with purified topoisomerase I and supercoiled plasmid DNA, followed by agarose gel electrophoresis to detect DNA relaxation or cleavage. IC50 values are calculated from dose-dependent inhibition of DNA relaxation.
|
| Cell Assay |
Cytotoxicity is assessed in cancer cell lines (e.g., L1210 leukemia, Walker 256 carcinosarcoma, lung, breast, colon cancer cells). Cells are seeded in 96-well plates, treated with serial dilutions of 7-Ethylcamptothecin for 48-72 hours, and cell viability is measured using MTT, MTS, or SRB assays. IC50 values are calculated from dose-response curves.
|
| Animal Protocol |
In vivo efficacy is evaluated in murine tumor models (e.g., L1210 leukemia, Walker 256 carcinosarcoma, xenograft models). 7-Ethylcamptothecin is administered via intravenous or intraperitoneal injection. Endpoints include tumor volume reduction, survival extension, and toxicity assessment.
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| ADME/Pharmacokinetics |
Molecular weight: 376.41; molecular formula: C22H20N2O4. Solubility: 10 mM in DMSO. Storage: powder at -20°C for 3 years, 4°C for 2 years; in solvent at -80°C for 6 months, -20°C for 1 month.
|
| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a camptothecin analogue, potential toxicities may include myelosuppression, gastrointestinal toxicity, and others typical of topoisomerase inhibitors. Standard toxicological studies would be required for drug development.
|
| References | |
| Additional Infomation |
7-Ethylcamptothecin is a pyranoindoquinoline compound.
7-Ethylcamptothecin is a research-grade compound, not approved for therapeutic use. It is primarily used as a lead compound for developing next-generation chemotherapeutic agents and camptothecin-based anticancer drugs. No FDA approval has been reported. Its mechanism involves Topo I inhibition. |
| Molecular Formula |
C22H20N2O4
|
|---|---|
| Molecular Weight |
376.4052
|
| Exact Mass |
376.142
|
| CAS # |
78287-27-1
|
| PubChem CID |
127584
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
752.9±60.0 °C at 760 mmHg
|
| Melting Point |
236-241ºC
|
| Flash Point |
409.1±32.9 °C
|
| Vapour Pressure |
0.0±2.6 mmHg at 25°C
|
| Index of Refraction |
1.713
|
| LogP |
2.6
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
28
|
| Complexity |
787
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)[C@@]4(CC)O)C2=NC5=CC=CC=C51
|
| InChi Key |
MYQKIWCVEPUPIL-QFIPXVFZSA-N
|
| InChi Code |
InChI=1S/C22H20N2O4/c1-3-12-13-7-5-6-8-17(13)23-19-14(12)10-24-18(19)9-16-15(20(24)25)11-28-21(26)22(16,27)4-2/h5-9,27H,3-4,10-11H2,1-2H3/t22-/m0/s1
|
| Chemical Name |
(19S)-10,19-diethyl-19-hydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4,6,8,10,15(20)-heptaene-14,18-dione
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~13.28 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 | 2.6567 mL | 13.2834 mL | 26.5668 mL | |
| 5 mM | 0.5313 mL | 2.6567 mL | 5.3134 mL | |
| 10 mM | 0.2657 mL | 1.3283 mL | 2.6567 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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