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Postion:Product Catalog >API>Antineoplastic agents>Natural sources of antineoplastic>7-Ethyl-10-hydroxycamptothecin
7-Ethyl-10-hydroxycamptothecin
  • 7-Ethyl-10-hydroxycamptothecin
  • 7-Ethyl-10-hydroxycamptothecin

7-Ethyl-10-hydroxycamptothecin NEW

Price $8 $3 $1
Package 1KG 25KG 100KG
Min. Order: 1KG
Supply Ability: g-kg-tons, free sample is available
Update Time: 2024-03-29

Product Details

Product Name: 7-Ethyl-10-hydroxycamptothecin CAS No.: 86639-52-3
Min. Order: 1KG Purity: 99%
Supply Ability: g-kg-tons, free sample is available Release date: 2024/03/29
Lead time: In stock, ready for shipment IIn stock, r: bag/bottle/drum/IBC
bag/bottle: By express, by air, by sea Origin: Manufacturer, advantage product
COA, MS: Available, contact us for details NAME: Sun

1. Materials information

Names

Name7-Ethyl-10-hydroxycamptothecin
SynonymMore Synonyms

 7-Ethyl-10-hydroxycamptothecin Biological Activity

DescriptionSN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
Related Catalog
Signaling Pathways >> Autophagy >> Autophagy
Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase
Research Areas >> Cancer
Target

Topoisomerase I

In VitroThe IC50 values for LoVo, HCT116, and HT29 cell lines is 20 nM, 50 nM, 130 nM, respectively. In all three SN-38 resistant cell lines Top1 activity is maintained in the presence of high concentrations of SN-38[2].
In VivoSN-38, the active and toxic metabolite of the anticancer prodrug Irinotecan. At 30 minutes after administration, Irinotecan plasma concentrations in Slco1a/1b(−/−) mice are 1.9-fold higher than in the wild-type mice (1.89 vs. 1.01 μM, respectively), whereas SN-38 plasma concentrations of Slco1a/1b(−/−) mice are 8-fold higher compare with wild-type mice (0.4 μg/mL vs. 0.05 μg/mL, respectively). Overall plasma exposure [AUC(5-240)] of Irinotecan is 1.7-fold higher in Oatp1a/1b knockout mice versus wild-type mice (209.8±6.7 vs. 120.9±4.4 μM/min; P<0.01), and 2.9-fold higher for SN-38 (50±2.9 vs. 12±2 μM/min; P<0.001)[3].
Kinase AssayLoVo, HCT116, and HT29 cell lines are trypsinized, resuspended and counted, and for each cell line 1 million cells are pipetted to each of three eppendorf tubes on ice. Cells are pelleted (5 min centrifugation, 300 g, 4°C) and snap-frozen in dry ice and ethanol and stored at -80°C until analysis. Nuclear extracts are prepared essentially, and Top1 activity measured in titration experiments with or without added SN-38 (at concentrations stated in the text) using the standard Rolling circle Enhanced Enzyme Activity Detection (REEAD) protocol. The activity is calculated in terms of numbers of Top1 specific signals relative to the amount of signals resulting from the addition a known concentration of control circles[2].
Cell AssayIn vitro SN-38 sensitivity is determined using the MTT assay. Cells are seeded in 96-well plates, and a range of SN-38 concentrations is added the following day. Following 48 h of drug exposure, the medium is discarded and the plates are incubated with medium containing MTT (0.5 mg/mL) for 3 h. Acidified (0.02 M HCl) sodium dodecyl sulphate (20 %) is added to dissolve the formed formazan. Optical density at 570 nm (and 670 nm for background) is measured, and the cell viability is calculated in percent compared to untreated cells. Experiments are repeated three times and the mean IC50 value ± standard deviation is determined. Relative resistance for each resistant cell line is calculated by dividing the mean IC50 value of the resistant cell line by the mean IC50 value of the corresponding parental cell line[2].
Animal AdminMice[3] Female wild-type, Slco1a/1b(−/−)(Oatp1a/1b knockout), Slco1a/1b(−/−);1B1(tg), and Slco1a/1b(−/−);1B3(tg) (liver-specific OATP1B1 and OATP1B3 humanized transgenic) mice of comparable genetic background (>99% FVB) between 8 and 14 weeks of age are used. Irinotecan (20 mg/mL in water-based solution containing NaOH, lactic acid, and sorbitol) is diluted with saline (to 2 mg/mL) for administration of 10 mg/kg; 5 μL/g bodyweight are administered intravenously to mice. SN-38 is dissolved in DMSO (1 mg/mL) and 1 μL/g body weight is administered intravenously to mice to achieve a dosage of 1 mg/kg. The experiments are terminated by isoflurane anaesthesia, heparin-blood sampling by cardiac puncture followed by cervical dislocation and tissue collection. Blood samples are centrifuged at 5,200 × g for 5 minutes at 4°C and plasma is collected and stored at −30°C until analysis.
References

[1]. Wallin A, et al. Anticancer effect of SN-38 on colon cancer cell lines with different metastatic potential. Oncol Rep. 2008 Jun;19(6):1493-8.

[2]. Jensen NF, et al. Characterization of DNA topoisomerase I in three SN-38 resistant human colon cancer cell lines reveals a newpair of resistance-associated mutations. J Exp Clin Cancer Res. 2016 Mar 31;35:56.

[3]. Stewart CF, et al. Disposition of irinotecan and SN-38 following oral and intravenous irinotecan dosing in mice. Cancer Chemother Pharmacol. 1997;40(3):259-65.

 Chemical & Physical Properties

Density1.5±0.1 g/cm3
Boiling Point810.3±65.0 °C at 760 mmHg
Melting Point217 °C
Molecular FormulaC22H20N2O5
Molecular Weight392.405
Flash Point443.8±34.3 °C
Exact Mass392.137207
PSA101.65000
LogP2.31
Vapour Pressure0.0±3.0 mmHg at 25°C
Index of Refraction1.738
Storage condition−20°C

2933399090

 Customs

HS Code2933399090
Summary2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

4-piperidin-1-ylpiperidine-1-carbonyl chloride,hydrochloride
MFCD08445613
[1,4'-Bipiperidine]-1'-carbonyl chloride, hydrochloride (1:1)
1,4'-Bipiperidine-1'-carbonyl chloride hydrochloride (1:1)
1-Chlorocarbonyl-4-piperidinopiperidine hydrochloride





2. Packaging of materials

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  • For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product. 

                             Or smaller package 1kg/bottle, 10kgs/bottle as request. 


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3. Shipping & Delivery

  • By Express

Provide door to door service

Suitable for goods under 50kg

Delivery: 3-7 days

Cost: low cost

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  • By Air

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Suitable for goods over 50kg

Delivery: 3-14 days

Cost: high cost

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  • By Sea

Provide seaport to seaport service

Suitable for goods over 100kg

Delivery: 2-45 days

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4. Contact information

For more details, pls contact us freely.

Email address: Sun@fdachem.com

Mob: 86 13526505137

WhatsApp/Skype/Wechat/LINE: 86 13526505137

















Company Profile Introduction

Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.

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  • Since: 2023-02-10
  • Address: Room 01, 2288 E05, Building 14, East Henan University, Science and Technology Park, 279 Xisanhuan Ro
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