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7-Ethylcamptothecin

CAS# 78287-27-1

7-Ethylcamptothecin

Catalog No. BCN2480----Order now to get a substantial discount!

Product Name & Size Price Stock
7-Ethylcamptothecin:5mg $39.00 In Stock
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Quality Control of 7-Ethylcamptothecin

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Chemical structure

7-Ethylcamptothecin

3D structure

Chemical Properties of 7-Ethylcamptothecin

Cas No. 78287-27-1 SDF Download SDF
PubChem ID 127584 Appearance Cryst.
Formula C22H20N2O4 M.Wt 376.41
Type of Compound Alkaloids Storage Desiccate at -20°C
Solubility DMSO : 5 mg/mL (13.28 mM; Need ultrasonic)
SMILES CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=CC=CC=C51
Standard InChIKey MYQKIWCVEPUPIL-QFIPXVFZSA-N
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Source of 7-Ethylcamptothecin

The barks of Camptotheca acuminata Decne

Biological Activity of 7-Ethylcamptothecin

Description7-Ethylcamptothecin has the superior antitumor activity than camptothecin, it has a stronger growth-inhibiting activity against tumor cells and remains in the intestinal tract for a longer time and in higher amounts when administered in vivo.
In vivo

Action of 7-ethylcamptothecin on tumor cells and its disposition in mice.[Pubmed: 3829011]

Cancer Treat Rep. 1987 Apr;71(4):341-8.

Some biological effects of camptothecin (CPT) and its new derivative 7-Ethylcamptothecin (ECPT) were studied. The drugs were effective against murine leukemia; 7-Ethylcamptothecin was more effective than CPT.
METHODS AND RESULTS:
Ip administration of 7-Ethylcamptothecin or CPT gave maximum treated/control values of 325% and 232%, respectively. The drugs also inhibited the growth of KB cells in vitro, 50% effective doses of 3.5 ng/ml of 7-Ethylcamptothecin and 8.6 ng/ml of CPT, indicating the stronger activity of ECPT. Pharmacokinetic studies of the drugs in mice showed that 7-Ethylcamptothecin had a longer biological half-life in the terminal phase and a larger amount remained in the plasma compared with CPT. After iv administration of 7-Ethylcamptothecin, the drug accumulated in the intestine, suggesting that the main route of excretion of the drug is through the biliary tract. The study on cell cycle progression by flow cytometry suggested that the main effect of both drugs on L1210 cells was the blocking of G2-M phase.
CONCLUSIONS:
These results suggest that the main reasons for the superior antitumor activity of 7-Ethylcamptothecin compared with CPT are as follows: (a) 7-Ethylcamptothecin had a stronger growth-inhibiting activity against tumor cells, and (b) 7-Ethylcamptothecin remained in the intestinal tract for a longer time and in higher amounts when administered in vivo.

Protocol of 7-Ethylcamptothecin

Kinase Assay

Partial purification and characterization of an esterase acting on the anticancer pro-drugs, 7-ethylcamptothecin derivatives.[Pubmed: 7492976]

Biol Pharm Bull. 1995 May;18(5):648-52.


METHODS AND RESULTS:
A hydrolytic enzyme which catalyzes hydrolysis of the ester-linkage of a series of 17-O-acyl derivatives of 7-Ethylcamptothecin-21-(2-dimethylamino)ethylamide [acyl derivatives of 22E] was purified from rat liver and its properties were characterized. It hydrolyzed the ester-linkage of all 22E derivatives tested as well as p-nitrophenyl acetate at pH 8-9 but had no effect on 7-ethyl-10-[4-(piperidino)-1-piperidino] carbonyloxycamptothecin (CPT-11: irinotecan), unlike CPT-11 converting carboxylesterase, which was previously purified from rat serum [Tsuji T. et al., J. Pharmacobio-Dyn., 14, 341 (1991)]. The enzyme had no effect on either acetyl choline or butyrylcholine. It was inhibited by several organophosphorous compounds such as diisopropyl fluorophosphate (DFP), bis-(p-nitrophenyl)phosphate and paraoxon, but was insensitive to inhibitors specific for choline esterases.
CONCLUSIONS:
These results indicate that this liver esterase is clearly distinct from choline esterase and serum CPT-11 converting enzyme and is able to convert pro-drugs, O-acyl derivatives of 22E, to an antitumor agent.

7-Ethylcamptothecin Dilution Calculator

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7-Ethylcamptothecin Molarity Calculator

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Preparing Stock Solutions of 7-Ethylcamptothecin

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6567 mL 13.2834 mL 26.5668 mL 53.1336 mL 66.4169 mL
5 mM 0.5313 mL 2.6567 mL 5.3134 mL 10.6267 mL 13.2834 mL
10 mM 0.2657 mL 1.3283 mL 2.6567 mL 5.3134 mL 6.6417 mL
50 mM 0.0531 mL 0.2657 mL 0.5313 mL 1.0627 mL 1.3283 mL
100 mM 0.0266 mL 0.1328 mL 0.2657 mL 0.5313 mL 0.6642 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on 7-Ethylcamptothecin

Action of 7-ethylcamptothecin on tumor cells and its disposition in mice.[Pubmed:3829011]

Cancer Treat Rep. 1987 Apr;71(4):341-8.

Some biological effects of camptothecin (CPT) and its new derivative 7-Ethylcamptothecin (ECPT) were studied. The drugs were effective against murine leukemia; ECPT was more effective than CPT. Ip administration of ECPT or CPT gave maximum treated/control values of 325% and 232%, respectively. The drugs also inhibited the growth of KB cells in vitro, 50% effective doses of 3.5 ng/ml of ECPT and 8.6 ng/ml of CPT, indicating the stronger activity of ECPT. Pharmacokinetic studies of the drugs in mice showed that ECPT had a longer biological half-life in the terminal phase and a larger amount remained in the plasma compared with CPT. After iv administration of ECPT, the drug accumulated in the intestine, suggesting that the main route of excretion of the drug is through the biliary tract. The study on cell cycle progression by flow cytometry suggested that the main effect of both drugs on L1210 cells was the blocking of G2-M phase. These results suggest that the main reasons for the superior antitumor activity of ECPT compared with CPT are as follows: (a) ECPT had a stronger growth-inhibiting activity against tumor cells, and (b) ECPT remained in the intestinal tract for a longer time and in higher amounts when administered in vivo.

Partial purification and characterization of an esterase acting on the anticancer pro-drugs, 7-ethylcamptothecin derivatives.[Pubmed:7492976]

Biol Pharm Bull. 1995 May;18(5):648-52.

A hydrolytic enzyme which catalyzes hydrolysis of the ester-linkage of a series of 17-O-acyl derivatives of 7-Ethylcamptothecin-21-(2-dimethylamino)ethylamide [acyl derivatives of 22E] was purified from rat liver and its properties were characterized. It hydrolyzed the ester-linkage of all 22E derivatives tested as well as p-nitrophenyl acetate at pH 8-9 but had no effect on 7-ethyl-10-[4-(piperidino)-1-piperidino] carbonyloxycamptothecin (CPT-11: irinotecan), unlike CPT-11 converting carboxylesterase, which was previously purified from rat serum [Tsuji T. et al., J. Pharmacobio-Dyn., 14, 341 (1991)]. The enzyme had no effect on either acetyl choline or butyrylcholine. It was inhibited by several organophosphorous compounds such as diisopropyl fluorophosphate (DFP), bis-(p-nitrophenyl)phosphate and paraoxon, but was insensitive to inhibitors specific for choline esterases. These results indicate that this liver esterase is clearly distinct from choline esterase and serum CPT-11 converting enzyme and is able to convert pro-drugs, O-acyl derivatives of 22E, to an antitumor agent.

Description

7-Ethylcamptothecin is one of camptothecin analogues. camptothecin (CPT), a cytotoxic alkaloid isolated from Camptotheca acuminate, is shown to have strong antitumor activity against L1210 leukemia and Walker 256 carcinosarcoma models.

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