| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
12-Ethyl-9-hydroxycamptothecin targets DNA topoisomerase I (Topo I), a crucial enzyme involved in DNA replication and transcription. It stabilizes the DNA-topoisomerase I complex, leading to DNA damage and apoptosis in rapidly dividing cells. The parent compound, Camptothecin, has an IC₅₀ of 679 nM for Topo I inhibition.
|
|---|---|
| ln Vitro |
12-Ethyl-9-hydroxycamptothecin is a camptothecin derivative.
In vitro, 12-Ethyl-9-hydroxycamptothecin exhibits strong anticancer activity by inhibiting DNA topoisomerase I. This leads to the stabilization of the cleavable complex, DNA damage, and the induction of apoptosis in cancer cells. It is widely used in both in vitro and in vivo research models to study colorectal cancer and other malignancies. |
| ln Vivo |
In vivo, 12-Ethyl-9-hydroxycamptothecin (SN38) is the active metabolite of irinotecan, a topoisomerase I inhibitor used in the treatment of colon and rectal cancer. It exhibits potent anticancer activity by inducing DNA damage and apoptosis in tumor cells.
|
| Enzyme Assay |
The inhibition of topoisomerase I by 12-Ethyl-9-hydroxycamptothecin is typically assessed using in vitro DNA relaxation assays. Purified topoisomerase I is incubated with supercoiled plasmid DNA in the presence of varying concentrations of the compound. The relaxation of the supercoiled DNA is analyzed by agarose gel electrophoresis.
|
| Cell Assay |
Cellular assays for 12-Ethyl-9-hydroxycamptothecin involve treating cancer cells with the compound and measuring cell viability, DNA damage, and apoptosis. Cell viability is assessed using MTT or CellTiter-Glo assays. DNA damage is measured by detecting γ-H2AX foci. Apoptosis is assessed by measuring caspase activity or Annexin V staining.
|
| Animal Protocol |
In vivo studies of 12-Ethyl-9-hydroxycamptothecin are conducted in mouse xenograft models of colorectal cancer and other malignancies. Tumor-bearing mice are administered the compound (or its prodrug irinotecan), and tumor growth inhibition is monitored.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of 12-Ethyl-9-hydroxycamptothecin (SN38) are well-characterized as the active metabolite of irinotecan. It has a short half-life and is primarily eliminated through biliary excretion. Its activity is influenced by the UGT1A1 polymorphism, which affects its glucuronidation and clearance.
|
| Toxicity/Toxicokinetics |
12-Ethyl-9-hydroxycamptothecin is intended for research use only and is not for therapeutic or diagnostic use in humans. Its toxicological profile is characterized by dose-limiting toxicities, including myelosuppression and severe diarrhea, which are associated with its active metabolite SN38.
|
| References | |
| Additional Infomation |
12-Ethyl-9-hydroxycamptothecin (SN38) is a DNA topoisomerase I inhibitor and the active metabolite of the anticancer drug irinotecan. It is widely used in research to study colorectal cancer and other malignancies. Its strong anticancer activity makes it a valuable tool for studying DNA damage and apoptosis.
|
| Molecular Formula |
C22H20N2O5
|
|---|---|
| Molecular Weight |
392.40
|
| Exact Mass |
392.137
|
| CAS # |
119577-28-5
|
| PubChem CID |
135423054
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
810.3±65.0 °C at 760 mmHg
|
| Flash Point |
443.8±34.3 °C
|
| Vapour Pressure |
0.0±3.0 mmHg at 25°C
|
| Index of Refraction |
1.738
|
| LogP |
2.31
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
29
|
| Complexity |
820
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CCC1=C2C(=C(C=C1)O)C=C3CN4C(=CC5=C(C4=O)COC(=O)[C@@]5(CC)O)C3=N2
|
| InChi Key |
KWUQFLSWWSXTSZ-QFIPXVFZSA-N
|
| InChi Code |
InChI=1S/C22H20N2O5/c1-3-11-5-6-17(25)13-7-12-9-24-16(19(12)23-18(11)13)8-15-14(20(24)26)10-29-21(27)22(15,28)4-2/h5-8,25,28H,3-4,9-10H2,1-2H3/t22-/m0/s1
|
| Chemical Name |
(19S)-5,19-diethyl-8,19-dihydroxy-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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : 83.33 mg/mL (212.36 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.30 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (5.30 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 | 2.5484 mL | 12.7421 mL | 25.4842 mL | |
| 5 mM | 0.5097 mL | 2.5484 mL | 5.0968 mL | |
| 10 mM | 0.2548 mL | 1.2742 mL | 2.5484 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
