10-Methoxycamptothecin is a natural bioactive analogue of camptothecin (CPT) extracted from Camptotheca acuminata and has been shown to have high anti-cancer properties. By measuring the anti-tumor activity against the 2774 cell line, 10-Methoxycamptothecin was found to be more cytotoxic than 10-hydroxycamptothecin.

Physicochemical Properties

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
Boiling Point	773.1±60.0 °C at 760 mmHg
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
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)

Biological Activity

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 rat plasma, and its major metabolite was confirmed to be 10-hydroxycamptothecin through HPLC/photodiode array detection (PDA) and LC-MS/MS analysis[1] 2. Detection-related pharmacokinetic supporting parameters: A validated RP-HPLC method with fluorescence detection was applied to determine the concentrations of 10-Methoxycamptothecin and its metabolite in rat plasma after intravenous administration; the calibration curves of 10-Methoxycamptothecin were linear (r² > 0.999) over the concentration ranges of 1.25–20 ng/mL and 20–320 ng/mL, the lower limit of quantification (LLOQ) for 10-Methoxycamptothecin with 0.1 mL plasma was 1.25 ng/mL, the accuracy of the detection method for 10-Methoxycamptothecin was 92.24–113.90%, the intra- and inter-day precision (RSD%) were ≤10.05%, and the mean recoveries of 10-Methoxycamptothecin at concentrations of 2.5 ng/mL, 40 ng/mL and 160 ng/mL were 95.09±3.94%, 98.67±1.40% and 95.65±2.15% respectively[1]
References	[1]. Development and validation of a RP-HPLC method with fluorescence detection for simultaneous determination of 10-methoxycamptothecin and its metabolite 10-hydroxycamptothecin in rat plasma. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Aug 15;903:81-7.
Additional Infomation	10-Methoxycamptothecin has been reported in Camellia sinensis, Perilla frutescens, and other organisms with data available. 1. 10-Methoxycamptothecin is a natural bioactive derivative of camptothecin (CPT) isolated from Camptotheca acuminata, and it has been confirmed to possess high anti-cancer properties[1]

Solubility Data

Solubility (In Vitro)

DMSO : ~8.33 mg/mL (~22.01 mM)

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. 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. 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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

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.