7-乙基-10-羟基喜树碱

7-Ethyl-10-Hydroxycamptothecin

	产品编号	CFN90335
	CAS编号	86639-52-3
	分子式 = 分子量	C₂₂H₂₀N₂O₅ = 392.4
	产品纯度	>=98%
	物理属性	Cryst.
	化合物类型	Alkaloids
	植物来源	The barks of Camptotheca acuminata Decne.
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产品名称	产品编号	CAS编号	包装	QQ客服
7-乙基-10-羟基喜树碱	CFN90335	86639-52-3	10mg	QQ客服：3257982914
7-乙基-10-羟基喜树碱	CFN90335	86639-52-3	20mg	QQ客服：3257982914
7-乙基-10-羟基喜树碱	CFN90335	86639-52-3	50mg	QQ客服：3257982914
7-乙基-10-羟基喜树碱	CFN90335	86639-52-3	100mg	QQ客服：3257982914

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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.

产品名称	产品编号	CAS编号	分子式 = 分子量	位单	联系QQ
10-甲氧基喜树碱; 10-Methoxycamptothecin	CFN90157	19685-10-0	C₂₁H₁₈N₂O₅ = 378.38	5mg	QQ客服：215959384
鲁比替康; Rubitecan	CFN93013	91421-42-0	C₂₀H₁₅N₃O₆ = 393.35	5mg	QQ客服：3257982914
10-硝基喜树碱; 10-Nitro-camptothecin	CFN90439	104195-61-1	C₂₀H₁₅N₃O₆ = 393.34	5mg	QQ客服：2056216494
盐酸拓扑替康; Topotecan hydrochloride	CFN90462	119413-54-6	C₂₃H₂₄ClN₃O₅ = 457.9	20mg	QQ客服：2159513211
盐酸依立替康; Irinotecan hydrochloride	CFN90886	100286-90-6	C₃₃H₃₉ClN₄O₆ = 623.2	20mg	QQ客服：1413575084
7-乙基喜树碱; 7-Ethylcamptothecin	CFN90336	78287-27-1	C₂₂H₂₀N₂O₄ = 376.41	20mg	QQ客服：2159513211
7-乙基-10-羟基喜树碱; 7-Ethyl-10-Hydroxycamptothecin	CFN90335	86639-52-3	C₂₂H₂₀N₂O₅ = 392.4	20mg	QQ客服：2159513211
9-甲氧基喜树碱; 9-Methoxycamptothecine	CFN99729	39026-92-1	C₂₁H₁₈N₂O₅ = 378.38	20mg	QQ客服：2159513211
9-氨基喜树碱; 9-Aminocamptothecin	CFN90309	91421-43-1	C₂₀H₁₇N₃O₄ = 363.37	20mg	QQ客服：2159513211
(S)-10-羟基喜树碱; (S)-10-Hydroxycamptothecin	CFN99735	19685-09-7	C₂₀H₁₆N₂O₅ = 364.35	20mg	QQ客服：2056216494

	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

7-乙基-10-羟基喜树碱

7-Ethyl-10-Hydroxycamptothecin

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