| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Animal Protocol |
1. Experimental animals: Male Wistar rats were selected as the experimental subjects for the pharmacokinetic study of 10-Methoxycamptothecin and its metabolite 10-hydroxycamptothecin
2. Administration mode: 10-Methoxycamptothecin was administered to rats via intravenous injection for subsequent plasma drug concentration detection and pharmacokinetic analysis[1] |
|---|---|
| ADME/Pharmacokinetics |
1. Metabolic characteristics: 10-methoxycamptothecin can be metabolized in mouse plasma. Its main metabolite was confirmed to be 10-hydroxycamptothecin by HPLC/photodiode array detection (PDA) and LC-MS/MS analysis [1]
2. Detection-related pharmacokinetic support parameters: The concentration of 10-methoxycamptothecin and its metabolites in mouse plasma after intravenous injection was determined by the validated RP-HPLC fluorescence detection method; The calibration curve of 10-methoxycamptothecin showed a linear relationship in the concentration range of 1.25–20 ng/mL and 20–320 ng/mL (r² > 0.999). When using 0.1 mL of plasma, the limit of quantitation (LLOQ) of 10-methoxycamptothecin was 1.25 ng/mL. The accuracy of the detection method for 10-methoxycamptothecin was 92.24–113.90%, and the intra-day and inter-day precision (RSD%) were both ≤10.05% at a concentration of 2.5 At concentrations of 10 ng/mL, 40 ng/mL, and 160 ng/mL, the average recoveries of 10-methoxycamptothecin were 95.09±3.94% and 98.67±1.40%, respectively. The recoveries were 95.65±2.15% [1]. |
| References | |
| Additional Infomation |
It has been reported that 10-methoxycamptothecin exists in tea (Camellia sinensis), perilla (Perilla frutescens), and other organisms with relevant data. 1. 10-methoxycamptothecin is a natural bioactive derivative of camptothecin (CPT) isolated from Camptotheca acuminata and has been shown to have high anticancer properties [1].
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| Molecular Formula |
C21H18N2O5
|
|---|---|
| Molecular Weight |
378.3780
|
| Exact Mass |
378.121
|
| CAS # |
19685-10-0
|
| PubChem CID |
97283
|
| Appearance |
White to yellow solid powder
|
| Density |
1.5±0.1 g/cm3
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| Boiling Point |
773.1±60.0 °C at 760 mmHg
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| Flash Point |
421.4±32.9 °C
|
| Vapour Pressure |
0.0±2.8 mmHg at 25°C
|
| Index of Refraction |
1.723
|
| LogP |
1.69
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
28
|
| Complexity |
790
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)N=C5C=CC(=CC5=C4)OC)O
|
| InChi Key |
KLFJSYOEEYWQMR-NRFANRHFSA-N
|
| InChi Code |
InChI=1S/C21H18N2O5/c1-3-21(26)15-8-17-18-12(6-11-7-13(27-2)4-5-16(11)22-18)9-23(17)19(24)14(15)10-28-20(21)25/h4-8,26H,3,9-10H2,1-2H3/t21-/m0/s1
|
| Chemical Name |
(19S)-19-ethyl-19-hydroxy-7-methoxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2(11),3,5,7,9,15(20)-heptaene-14,18-dione
|
| 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: 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 : ~8.33 mg/mL (~22.01 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 0.83 mg/mL (2.19 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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 0.83 mg/mL (2.19 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 8.3 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. View More
Solubility in Formulation 3: ≥ 0.83 mg/mL (2.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6428 mL | 13.2142 mL | 26.4285 mL | |
| 5 mM | 0.5286 mL | 2.6428 mL | 5.2857 mL | |
| 10 mM | 0.2643 mL | 1.3214 mL | 2.6428 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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