IR 783
目录号 : GC48378
A fluorescent probe for in vivo tumor cell imaging
Cas No.:115970-66-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IR 783 is a heptamethine cyanine fluorescent probe for in vivo imaging of tumor cells.1,2 It displays excitation/emission maxima of 633/780 nm, respectively. IR 783 is transported into tumor cells, an effect that can be blocked by the organic anion transporting polypeptide (OATP) inhibitor sulfobromophthalein .1 In vivo, IR 783 (11.25 mg/kg) preferentially accumulates in tumor tissue in an ACHN kidney cancer mouse xenograft model.2 It has been conjugated to polyethylenimines for tumor-specific gene delivery.3
1.Yuan, J., Yi, X., Yan, F., et al.Near?infrared fluorescence imaging of prostate cancer using heptamethine carbocyanine dyesMol. Med. Rep.11(2)821-828(2015) 2.Yang, X., Shao, C., Wang, R., et al.Optical imaging of kidney cancer with novel near-infrared heptamethine carbocyanine fluorescent dyesJ. Urol.189(2)702-710(2013) 3.De Los Reyes-Berbel, E., Salto-Gonzalez, R., Ortega-MuÑoz, M., et al.PEI-NIR heptamethine cyanine nanotheranostics for tumor targeted gene deliveryBioconjug. Chem.29(8)2561-2575(2018)
| Cas No. | 115970-66-6 | SDF | |
| Canonical SMILES | ClC1=C(CCC/C1=C\C=C2C(C)(C)C3=CC=CC=C3N\2CCCCS([O-])(=O)=O)/C=C/C4=[N+](CCCCS([O-])(=O)=O)C5=CC=CC=C5C4(C)C.[Na+] | ||
| 分子式 | C38H46ClN2O6S2•Na | 分子量 | 749.4 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 1 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3344 mL | 6.672 mL | 13.344 mL |
| 5 mM | 0.2669 mL | 1.3344 mL | 2.6688 mL |
| 10 mM | 0.1334 mL | 0.6672 mL | 1.3344 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Synthesis and Biological Evaluation of Genistein-IR783 Conjugate: Cancer Cell Targeted Delivery in MCF-7 for Superior Anti-Cancer Therapy
Molecules 2019 Nov 14;24(22):4120.PMID:31739548DOI:10.3390/molecules24224120.
The flavonoid-based natural product genistein is a biologically active compound possessing promising anti-oxidant and anti-cancer properties. Poor pharmacokinetics along with low potency limit however the therapeutic application of genistein in cancer therapy. In order to overcome those limitations and to expand its therapeutic window of efficacy, we sought to covalently attach genistein with a heptamethine cyanine dye-IR 783-for cancer cell targeting and enhanced delivery to tumors. Herein we report the synthesis, a selective detailed characterization and preliminary in vitro/in vivo biological evaluation of genistein-IR 783 conjugate 4. The conjugate 4 displayed improved potency against human breast cancer MCF-7 cells (10.4 ± 1.0 μM) as compared with the parent genistein (24.8 ± 0.5 μM) or IR 783 (25.7 ± 0.7 μM) and exhibited selective high uptake in MCF-7 as against the normal mammary gland MCF-10A cells in various assays. In the cell viability assay, conjugate 4 exhibited over threefold lower potency against MCF-10A cells (32.1 ± 1.1 μM) suggesting that the anti-cancer profile of parent genistein is significantly improved upon conjugation with the dye IR783. Furthermore, the genistein-IR783 conjugate 4 was shown to be especially accumulated in MCF-7 cancer cells by fluorescent intensity measurements and inverted fluorescence microscopy in fixed cells as well as in live cells with time via live cell confocal fluorescence imaging. The mechanism-based uptake inhibition of conjugate 4 was observed with OATPs inhibitor BSP and in part with amiloride, as a macropinocytosis inhibitor. For the first time we have shown amiloride inhibited uptake of cyanine dye by about ~40%. Finally, genistein-IR 783 conjugate 4 was shown to be localized in MCF-7 tumor xenografts of mice breast cancer model via in vivo near infrared fluorescence (NIRF) imaging. In conclusion, conjugation of genistein with cyanine dye IR783 indeed improved its pharmacological profile by cancer cell selective uptake and targeting and therefore warrants further investigations as a new anti-cancer therapeutics derived from natural product genistein.