规格 | 价格 | |
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500mg | ||
1g | ||
Other Sizes |
靶点 |
Radionuclide-Drug Conjugates (RDCs)
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体外研究 (In Vitro) |
[111-二乙烯三胺五乙酸-D-Phe1]-奥曲肽(DTPA-octreotide)闪烁扫描术已被广泛接受为肿瘤学中用于成像生长抑素受体阳性肿瘤的诊断临床程序。然而,铟-111作为放射性标记有几个缺点,包括可用性有限、伽马能量次优和患者的高辐射负担。我们最近报道了99mTc-EDDA/HYNIC-TOC的临床前开发,这是一种新的奥曲肽衍生物,在体外显示出有希望的结果[1]。
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体内研究 (In Vivo) |
我们现在报告了我们在10名肿瘤患者中使用这种新型放射性药物的初步临床经验。临床诊断为:类癌综合征(n=5)、甲状腺癌症(n=3)、癌症(n=1)和垂体瘤(n=1。对6例99mTc-EDDA/HYNIC-TOC的生物分布和动力学与111In-DTPA-octreotide进行了比较,5例与111In-DOTA-TOC进行了比较。使用新的示踪剂,肿瘤在注射后15分钟内成像,并在注射后4小时显示出最高的靶/非靶比。肿瘤摄取持续20小时p.i。血液清除率与111In-DTPA-奥曲肽相似,但比111In-DOTA-TOC快,而尿排泄量低于111In衍生物。半定量感兴趣区域分析表明,99mTc-EDDA/HYNIC-TOC比111In衍生物产生更高的肿瘤/器官(靶/非靶)比率,特别是在心脏和肌肉方面。在99mTc图像中可以检测到更多的病变。我们得出结论,与目前可用的111In标记的奥曲肽衍生物相比,99mTcEDDA/HYNIC-TOC在鉴定生长抑素受体阳性肿瘤部位方面显示出更好的成像特性[1]。
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动物实验 |
Patients: This clinical study was approved by the local ethical committee and all patients gave their informed consent prior to inclusion. Scintigraphy with 99mTc-EDDA/HYNIC-TOC was performed in ten patients, details of whom are given in Table 1. Comparative imaging with 111In-DTPA-octreotide alone was performed in five patients and with 111In-DOTA-TOC alone in four patients, while one patient underwent all three imaging modalities. The time between comparative studies normally ranged from 2 to 30 days, although in one patient the 111In study was performed on the day following the 99mTc study. Patients were not treated with cold somatostatin analogues within 1 month before the imaging studies. Imaging. Planar imaging was performed with a double-head camera (Elscint HELIX, Haifa, Israel). All patients were imaged at 4 h post injection. Seven patients were additionally imaged at 1–2 h, and in two patients additional imaging was performed at 15 min and 20 h. For 99mTc studies the camera was equipped with a lowenergy all-purpose parallel-hole collimator, window setting 140 keV, width 10%. 111In images were obtained using a high-energy parallel-hole collimator, with window setting over both 111In peaks at 172 and 246 keV and a window width of 20%. Single-photon emission tomography (SPET) imaging of areas of interest was performed 4 h post injection and in some patients additionally at 20 h. For 99mTc tomographic acquisition, the same double-head camera as described above was used. Acquisition parameters were: 60 projections, 25 s/projection, matrix 64×64, zoom 1. SPET for 111In studies was performed on a Siemens single-head camera (ZL3000, Siemens, Erlangen, Germany) equipped with a medium-energy parallel-hole collimator using 60 projections, 35 s/projection, matrix 64×64. This camera system was also used for SPET of brain and neck regions of interest (ROIs) for 99mTc studies using a low-energy parallel-hole collimator. In general, imaging parameters were chosen that produced comparable whole-body counts for both 111In and 99mTc studies. Total whole-body counts (arithmetic mean of anterior and posterior images ± SD) were 2056±244 kcounts for 111In studies and 1764±428 kcounts for 99mTc studies (decay-corrected to the time of injection).
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参考文献 | |
其他信息 |
The imaging properties of 99mTc-EDDA/HYNIC-TOC appear to be advantageous for investigating somatostatin receptor-positive tumours in man. This new preparation has a rapid tumour uptake and a similar biodistribution to 111In-DTPA-octreotide but produced higher tumour to organ ratios and detected a greater number of lesions. Finally, the easy availability of 99mTc from generators and the low cost of this radionuclide make 99mTc-EDDA/ HYNIC-TOC a promising candidate to replace currently used 111In-octreotide derivatives in diagnostic nuclear medicine in oncology. [1]
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分子式 |
C55H71N13O12S2
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分子量 |
1170.36
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精确质量 |
1169.48
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元素分析 |
C, 56.44; H, 6.11; N, 15.56; O, 16.40; S, 5.48
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CAS号 |
257943-19-4
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序列 |
{Hynic}-{d-Phe}-Cys-Tyr-{d-Trp}-Lys-Thr-Cys-{Thr-ol} (Disulfidebridge:Cys2-Cys7);
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短序列 |
FCYWKTCT; {Hynic}-{d-Phe}-CY-{d-Trp}-KTC-{Thr-ol} (Disulfidebridge:Cys2-Cys7)
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外观&性状 |
Typically exists as solid at room temperature
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SMILES |
S1C([H])([H])[C@@]([H])(C(N([H])[C@]([H])(C([H])([H])O[H])[C@@]([H])(C([H])([H])[H])O[H])=O)N([H])C([C@]([H])([C@@]([H])(C([H])([H])[H])O[H])N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])N([H])C([C@@]([H])(C([H])([H])C2=C([H])N([H])C3=C([H])C([H])=C([H])C([H])=C23)N([H])C([C@@]([H])(C([H])([H])C2C([H])=C([H])C(=C([H])C=2[H])O[H])N([H])C([C@]([H])(C([H])([H])S1)N([H])C([C@@]([H])(C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])N([H])C(C1=C([H])N=C(C([H])=C1[H])N([H])N([H])[H])=O)=O)=O)=O)=O)=O)=O
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别名 |
HYNIC-Tyr3-octreotide; Hynic-toc; XBO8UII5SV; Hydrazinonicotinyl-Tyr3-octreotide; UNII-XBO8UII5SV; 913556-62-4; N-((6-Hydrazinyl-3-pyridinyl)carbonyl)-D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-threonyl-N-((1R,2R)-2-hydroxy-1-(hydroxymethyl)propyl)-L-cysteinamide cyclic (2->7)-disulfide;
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外实验) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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溶解度 (体内实验) |
注意: 如下所列的是一些常用的体内动物实验溶解配方,主要用于溶解难溶或不溶于水的产品(水溶度<1 mg/mL)。 建议您先取少量样品进行尝试,如该配方可行,再根据实验需求增加样品量。
注射用配方
注射用配方1: DMSO : Tween 80: Saline = 10 : 5 : 85 (如: 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *生理盐水/Saline的制备:将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中,得到澄清溶液。 注射用配方 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (如: 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 注射用配方 3: DMSO : Corn oil = 10 : 90 (如: 100 μL DMSO → 900 μL Corn oil) 示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液,加到 900 μL Corn oil/玉米油中, 混合均匀。 View More
注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如:100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)] 口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠) 口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素) 示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中,得到0.5%CMC-Na澄清溶液;然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中,得到悬浮液。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 0.8544 mL | 4.2722 mL | 8.5444 mL | |
5 mM | 0.1709 mL | 0.8544 mL | 1.7089 mL | |
10 mM | 0.0854 mL | 0.4272 mL | 0.8544 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。