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7-Ethyl-10-Hydroxycamptothecin
7-Ethyl-10-Hydroxycamptothecin
ChemFaces products have been cited in many studies from excellent and top scientific journals
Product Name 7-Ethyl-10-Hydroxycamptothecin
Price: $30 / 20mg
CAS No.: 86639-52-3
Catalog No.: CFN90335
Molecular Formula: C22H20N2O5
Molecular Weight: 392.4 g/mol
Purity: >=98%
Type of Compound: Alkaloids
Physical Desc.: Cryst.
Source: The barks of Camptotheca acuminata Decne.
Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download: COA    MSDS    SDF
Similar structural: Comparison (Web)  (SDF)
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Related Screening Libraries
Size /Price /Stock 10 mM * 100 uL in DMSO / Inquiry / In-stock
10 mM * 1 mL in DMSO / Inquiry / In-stock
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Biological Activity
Description: 7-Ethyl-10-hydroxycamptothecin shows cytotoxicity against breast cancer, it efficiently target-bind to the colon and lungs of mice.
Targets: P-gp
In vitro:
Nanotechnology. 2013 Jun 21;24(24):245101.
Mechanisms of chitosan-coated poly(lactic-co-glycolic acid) nanoparticles for improving oral absorption of 7-ethyl-10-hydroxycamptothecin.[Pubmed: 23702815]
Chitosan-modified poly(lactic-co-glycolic acid) nanoparticles (CHI/PLGA NPs) loaded with 7-Ethyl-10-Hydroxycamptothecin (SN-38), named CHI/PLGA/SN-38 NPs, were successfully prepared using an oil-in-water (O/W) solvent evaporation method.
METHODS AND RESULTS:
The physicochemical properties of the novel NPs were characterized by DLS, Zeta potential, SEM, DSC, XRD, and FTIR. The encapsulation efficiency and drug loading content were 71.83 (±2.77)% and 6.79 (±0.26)%, respectively. In vitro drug release in the simulated gastric juice was lower than that in the intestinal juice. In situ single-pass intestinal perfusion (SPIP) studies indicated a dramatic improvement of drug absorption as a result of the synergistic effect between CHI and PLGA on P-glycoprotein (Pgp) inhibition. CHI/PLGA NPs showed high cellular uptake and low efflux for drugs in Caco-2 cells. The cytotoxicity studies revealed that CHI/PLGA NPs had a transient effect on the membrane integrity, but did not have an influence on cell viability. Based on the in vitro release studies, SPIP, and intracellular drug accumulation and transport investigations, we speculate rationally that CHI/PLGA NPs were mainly internalized in the form of intact NPs, thus escaping the recognition of enterocyte Pgp and avoiding efflux into the apical part of the enterocytes. After partial release of drugs inside the enterocytes, CHI/PLGA interfered with the microenvironment of Pgp and further weakened the Pgp-mediated efflux. Then, the drug-loaded NPs exited via the exocytose effect from the basal part of the enterocytes and entered the blood circulation.
CONCLUSIONS:
These results showed that CHI/PLGA NPs would be smart oral delivery carriers for antineoplastic agents that are also Pgp substrates.
In vivo:
Yao Xue Xue Bao. 2014 Jul;49(7):1029-33.
Pharmacokinetics of SN-38 in rats and tissue distribution of 7-ethyl-10-hydroxycamptothecin in mice after intravenous injection of irinotecan hydrochloride nanoparticles.[Pubmed: 25233635]
The paper reported an investigation of the pharmacokinetics of SN-38 (7-Ethyl-10-Hydroxycamptothecin) in rats and the tissue distribution in mice after injection of irinotecan hydrochloride nanoparticles (CPT-11) via tail veins. An LC-MS/MS method was established to determine the concentrations of 7-Ethyl-10-Hydroxycamptothecin in whole blood of rats and in different tissues of mice.
METHODS AND RESULTS:
The pharmacokinetics and tissue distribution of 7-Ethyl-10-Hydroxycamptothecin were compared after the intravenous injection of CPT-11 NPs and CPT-11 solution. Compared with irinotecan solution, the elimination half-life of 7-Ethyl-10-Hydroxycamptothecin was prolonged from 2.17 h to 2.67 h after the intravenous injection of CPT-11 NPs, but its AUC had little change. After the injection of CPT-11 NPs in mice, over time, the concentrations of CPT-11-metabolized 7-Ethyl-10-Hydroxycamptothecin in CPT-11 NPs were significantly higher in the whole blood, colon and lungs than those in CPT-11 solution, followed by in the spleen and liver, but those in the heart and brain had no change. However, the amount of 7-Ethyl-10-Hydroxycamptothecin in the kidneys was reduced with time. CPT-11 NPs could prolong 7-Ethyl-10-Hydroxycamptothecin's (one of its metabolites) blood circulation time in rats and significantly increased the concentration of CPT-11-metabolized 7-Ethyl-10-Hydroxycamptothecin in the whole blood, colon and lungs of mice.
CONCLUSIONS:
CPT-11 NPs made 7-Ethyl-10-Hydroxycamptothecin efficiently target-bind to the colon and lungs of mice.
7-Ethyl-10-Hydroxycamptothecin Description
Source: The barks of Camptotheca acuminata Decne.
Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).

Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

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Calculate Dilution Ratios(Only for Reference)
1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5484 mL 12.7421 mL 25.4842 mL 50.9684 mL 63.7105 mL
5 mM 0.5097 mL 2.5484 mL 5.0968 mL 10.1937 mL 12.7421 mL
10 mM 0.2548 mL 1.2742 mL 2.5484 mL 5.0968 mL 6.371 mL
50 mM 0.051 mL 0.2548 mL 0.5097 mL 1.0194 mL 1.2742 mL
100 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.5097 mL 0.6371 mL
* Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
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