Vipivotide-tetraxetan-PSMA-617-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVipivotide tetraxetanCat. No.: HY-117410CAS No.: 1702967-37-0Synonyms: PSMA-617分式: CHNO分量: 1042.14作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg/mL (119.95 mM;

2、 Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 0.9596 mL 4.7978 mL 9.5956 mL5 mM 0.1919 mL 0.9596 mL 1.9191 mL10 mM 0.0960 mL 0.4798 mL 0.9596 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)

3、儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (2.00 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (2.00 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecul

4、es 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (2.00 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Vipivotide tetraxetan (PSMA-617)是前列腺特異性膜抗原 (PSMA) 的強(qiáng)有效抑制劑，其 Ki 值為 0.37 nM。IC50 & Target Ki: 0.37 nM (PSMA) 1.體外研究 Vipivotide tetraxetan (PSMA-617) demonstrates high radiolytic stability for at least 72 h. A

5、high inhibitionpotency (equilibrium dissociation constant Ki=2.342.94 nM on LNCaP; Ki=0.370.21 nM enzymaticallydetermined) and highly efficient internalization into LNCaP cells are demonstrated 1.體內(nèi)研究 Organ distribution with 68Ga-labeled Vipivotide tetraxetan (PSMA-617) after 1 h (n=3) reveals a hig

6、h specificuptake in LNCaP tumors and in the kidneys. The high uptake in the kidneys is nearly completely blocked bycoinjection of 2 mg of 2-PMPA per kilogram. Other organs such as the liver, lung, and spleen show rather lowuptake and no blocking effect, with the exception of the spleen. Tumor-to-bac

7、kground ratios are 7.8 (tumor toblood) and 17.1 (tumor to muscle) at 1 h after injection. As compared with the 68Ga-labeled version, theorgan distribution with 177Lu-labeled Vipivotide tetraxetan (PSMA-617) (n=3) show a similar uptake in theLNCaP tumors and in the kidneys. The liver uptake is found

8、to be statistically different. Tumor-to-backgroundratios determined 1 h after injection show slightly higher values (tumor to blood, 22.1; tumor to muscle, 25.6)than previous organ distribution with 68Ga-labeled Vipivotide tetraxetan (PSMA-617) 1.REFERENCES1. Beneov M, et al. Preclinical Evaluation of a Tailor-Made DOTA-Conjugated PSMA Inhibitor with Optimized Linker Moiety for Imagingand Endoradiotherapy of Prostate Cancer. J Nucl Med. 2015 Jun;56(6):914-20.McePdfHeightCaution: Product has not been fully validated for medical appl