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EC-17 disodium salt Sale

(Synonyms: 5-[[[[2-[[(4S)-4-[[4-[[(2-氨基-1,4-二氢-4-氧代-6-蝶啶基)甲基]氨基]苯甲酰基]氨基]-4-羧基-1-氧代丁基]氨基]乙基]氨基]硫代甲酰]氨基]-2-(6-羟基-3-氧代-3H-氧杂蒽-9-基)苯甲酸钠盐) 目录号 : GC34017

EC-17(disodiumsalt)是一种叶酸受体α(FRα)的靶向造影剂,在可见光谱中具有荧光特性。EC-17的激发和发射波长为470/520nm。

EC-17 disodium salt Chemical Structure

Cas No.:910661-33-5

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1mg
¥3,060.00
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5mg
¥7,650.00
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Sample solution is provided at 25 µL, 10mM.

Description

EC-17 (disodium salt) is a folate receptor alpha (FRα) targeting contrast agent with fluorescent properties in the visible light spectrum. The peak excitation and emission wavelengths of EC-17 are 470/520 nm.

EC-17 contains the fluorescein fluorochrome and has a spectral wavelength of 490-530 nm. EC-17 is synthesized by a folate (vitamin B9) and fluorescein isothiocyanate (FITC) conjugated through an ethylenediamine spacer to produce folate-FITC, with a molecular weight of 917 kDa. FITC is a derivative of fluorescein functionalized with an isothiocyanate reactive group. The folate-FITC conjugate forms a negatively charged fluorescent molecule that specifically targets cell-surface FRα and is subsequently internalized into the cytoplasm. The signal-to-background ratio (SBR) of EC-17 for HeLa cells range from 0.97 to 7.32 depending on the molarity and concentration of cancer cells[1].

The mean fluorescence signal from the animals injected with EC-17 to be 42,234 ± 12,234 au[1]. Fluorescence microscopy for folate-FITC shows a strong signal in all malignant tumors with FR-α expression and no signal in FR-α-negative malignant or benign lesions[2].

[1]. Tummers QR, et al. Intraoperative imaging of folate receptor alpha positive ovarian and breast cancer using the tumor specific agent EC17. Oncotarget. 2016 May 31;7(22):32144-55.

实验参考方法

Cell experiment:

KB, HeLa, and TC1 cells are plated on a cell culture treated 6-well plate and incubated for 16 hours. Once confluent, EC-17 is added cells. The cells are incubated and sealed in a light-protected environment for 45 minutes. Cells are then washed 3 times with PBS and plated and underwent fluorescence microscopy[1].

Animal experiment:

Mice[1]Mice are injected subcutaneously in the flank with 1.2×106 TC1 cells (C57BL/6 mice), 1.0×106 HeLa cells (NOD.Cg-Prkdcscid  Il2rgtm1Wjl/SzJ mice), or 1.0×106 KB cells (NOD.Cg-Prkdcscid, Il2rgtm1Wjl/SzJ mice). Once tumor volume reached approximately 300 mm3 half of the mice are injected with 0.1 mg/kg of EC-17 and the other half with 0.1 mg/kg of OTL38 via tail vein. Three hours later, the fluorescence of tumors is measured using Flocam[1].

References:

[1]. Tummers QR, et al. Intraoperative imaging of folate receptor alpha positive ovarian and breast cancer using the tumor specific agent EC17. Oncotarget. 2016 May 31;7(22):32144-55.

化学性质

Cas No. 910661-33-5 SDF
别名 5-[[[[2-[[(4S)-4-[[4-[[(2-氨基-1,4-二氢-4-氧代-6-蝶啶基)甲基]氨基]苯甲酰基]氨基]-4-羧基-1-氧代丁基]氨基]乙基]氨基]硫代甲酰]氨基]-2-(6-羟基-3-氧代-3H-氧杂蒽-9-基)苯甲酸钠盐
Canonical SMILES S=C(NCCNC(CC[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CN=C3N=C(N)NC(C3=N2)=O)C=C1)=O)=O)NC4=CC5=C(C6(C7=C(OC8=C6C=CC(O)=C8)C=C(O)C=C7)OC5=O)C=C4.[Na+]
分子式 C42H36N10NaO10S+ 分子量 895.85
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.1163 mL 5.5813 mL 11.1626 mL
5 mM 0.2233 mL 1.1163 mL 2.2325 mL
10 mM 0.1116 mL 0.5581 mL 1.1163 mL
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