SN-38 - Moligand™, 10mM in DMSO , CAS No.86639-52-3

CAS: 86639-52-3 Cat. No.: S407944 分子式: C₂₂H₂₀N₂O₅ 分子量: 392.4 EC番号: 643-093-9

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

NK012 | 1H-Pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, 4,11-diethyl-4,9-dihydroxy-, (4S)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

SN-38 (NK012) is an active metabolite of CPT-11, inhibitsDNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 inducesautophagy.
In vitro

SN-38, a biological active metabolite of irinotecan hydrochloride (CPT-11). SN-38 causes the strongest inhibition of DNA topoisomerase I, followed by CPT and then CPT-11. CPT-11 dose dependently shifts the position of relaxed DNA in the direction of nicked DNA, but SN-38 and CPT shows no effect on the position of relaxed DNA. SN-38 dose-dependently and time-dependently inhibit DNA synthesis. Respective IC50 values of SN-38, in DNA synthesis is 0.077 μM. The inhibitory effect of SN-38 on RNA synthesis is less than that on DNA synthesis and it does not inhibit protein synthesis. SN-38 caused frequent DNA single-strand breaks in P388 cells.

In vivo

After oral dosing, peak SN-38 concentrations occurrs within 1 h, and the The percent unbound SN-38 lactone in murine plasma at 1000 ng/mL is 3.4 +/- 0.67%, whereas at 100 ng/mL the percent unbound is 1.18 +/- 0.14%. SN-38 lactone AUCs in micebearing human neuroblastoma xenografts are greater than in nontumor-bearing animals.
Cell Data

cell lines：

Concentrations：0 -1000 nM

Incubation Time：48 h

Powder Purity:≥99%

Specifications

同義語

NK012 | 1H-Pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, 4,11-diethyl-4,9-dihydroxy-, (4S)-

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

名前と識別子

• 異性体SMILES: CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)[C@@]4(CC)O)C2=NC5=C1C=C(C=C5)O
• WGKドイツ: 3
• RTECS: UQ0491000
• 代替CAS番号: 86639-52-3
• NSC番号: 673596
• MeSH用語: 7 Ethyl 10 hydroxycamptothecin;7-ethyl-10-hydroxycamptothecin;Camptosar;Camptothecin 11;camptothecin-11;CPT 11;CPT-11;CPT11;irinotecan;irinotecan hydrochloride;Irrinotecan;NK012 compound;SN 38;SN 38 11;SN-38;SN-38-11;SN3811
• 分子量: 392.4
• Reaxy-Rn: 4279374
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4279374&ln=

関連ターゲット（人間）

TOP1 Tclin DNA topoisomerase 1 (0 Activities)

Discover Target: TOP1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABCG2 Tchem ATP-binding cassette sub-family G member 2 (0 Activities)

Discover Target: ABCG2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

化学的性質と物理的性質

• 溶解度: Solubility (25°C) In vitro DMSO: 71 mg/mL (200.92 mM); Ethanol: 50 mg/mL (141.49 mM); Water: Insoluble
• 比旋光度［α］: +20.0 to +30.0 deg(C=0.2, THF)
• 融点（°C）: 217°C

参考文献

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