Vipivotide tetraxetan (PSMA-617)是一种靶向前列腺特异性膜抗原（PSMA；Ki=0.37nM）的合成配体分子。
Cas No.:1702967-37-0
Sample solution is provided at 25 µL, 10mM.
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Vipivotide tetraxetan (PSMA-617) is a synthetic ligand molecule that targets the prostate-specific membrane antigen (PSMA; Ki=0.3nM)[1-2]. Vipivotide tetraxetan can be chelated with 68G or 177Lu for the diagnosis and targeted therapy research of metastatic castration-resistant prostate cancer (mCRPC)[3-4].
In vitro, PC3-PSMA and LNCaP prostate cancer cell lines were pretreated with 5-aza-2'-deoxycytidine (5-aza-dC) and valproic acid (VPA) for 5 days, followed by co-incubation with ¹⁷⁷Lu-chelated Vipivotide tetraxetan (50kBq/1 mL) for 1-24 hours. 5-aza-dC and VPA significantly increased the cellular uptake of Vipivotide tetraxetan[5]. PSMA-positive PC-3 PIP tumor cells were treated with ¹⁶¹Tb- or ¹⁷⁷Lu-labeled Vipivotide tetraxetan (0.1-10MBq/mL) for 4 hours. ¹⁶¹Tb- or ¹⁷⁷Lu-labeled Vipivotide tetraxetan significantly reduced cell viability and survival[6].
In vivo, BALB/c nude mice bearing HepG2 hepatocellular carcinoma xenografts were treated with a single intravenous injection of ¹⁷⁷Lu-labeled Vipivotide tetraxetan (37MBq per mouse). ¹⁷⁷Lu-labeled Vipivotide tetraxetan significantly inhibited tumor growth and prolonged the survival of the tumor-bearing mice[7]. BALB/cAnNRj mice were treated with a single intravenous injection of ¹⁷⁷Lu-labeled Vipivotide tetraxetan (120, 160, or 200MBq per mouse). ¹⁷⁷Lu-labeled Vipivotide tetraxetan caused transient hematological toxicity (including decreased counts of white blood cells, red blood cells, and platelets) but did not cause death[8].
References:
[1] Benešová M, Schäfer M, Bauder-Wüst U, et al. Preclinical Evaluation of a Tailor-Made DOTA-Conjugated PSMA Inhibitor with Optimized Linker Moiety for Imaging and Endoradiotherapy of Prostate Cancer. J Nucl Med. 2015 Jun;56(6):914-20.
[2] Ruigrok EAM, van Vliet N, Dalm SU, et al. Extensive preclinical evaluation of lutetium-177-labeled PSMA-specific tracers for prostate cancer radionuclide therapy. Eur J Nucl Med Mol Imaging. 2021 May;48(5):1339-1350.
[3] Han XD, Liu C, Liu F, et al. 64Cu-PSMA-617: A novel PSMA-targeted radio-tracer for PET imaging in gastric adenocarcinoma xenografted mice model. Oncotarget. 2017 May 26;8(43):74159-74169.
[4] Vilangattil MM, Swaidan A, Godinez J, et al. Hematological toxicity of [225Ac]Ac-PSMA-617 and [177Lu]Lu-PSMA-617 in RM1-PGLS syngeneic mouse model. EJNMMI Radiopharm Chem. 2025 Mar 24;10(1):12.
[5] Runge R, Naumann A, Miederer M, et al. Up-Regulation of PSMA Expression In Vitro as Potential Application in Prostate Cancer Therapy. Pharmaceuticals (Basel). 2023 Apr 4;16(4):538.
[6] Müller C, Umbricht CA, Gracheva N, et al. Terbium-161 for PSMA-targeted radionuclide therapy of prostate cancer. Eur J Nucl Med Mol Imaging. 2019 Aug;46(9):1919-1930.
[7] Lu Q, Long Y, Gai Y, et la. [177Lu]Lu-PSMA-617 theranostic probe for hepatocellular carcinoma imaging and therapy. Eur J Nucl Med Mol Imaging. 2023 Jul;50(8):2342-2352.
[8] Kristiansson A, Vilhelmsson Timmermand O, Altai M, et al. Hematological Toxicity in Mice after High Activity Injections of 177Lu-PSMA-617. Pharmaceutics. 2022 Mar 28;14(4):731.
Vipivotide tetraxetan (PSMA-617)是一种靶向前列腺特异性膜抗原（PSMA；Ki=0.37nM）的合成配体分子[1-2]。Vipivotide tetraxetan可与68Gu或177Lu螯合，用于PSMA阳性转移性去势抵抗性前列腺癌（mCRPC）的诊断与靶向治疗研究[3-4]。
在体外，5-aza-2‘-deoxycytidine （5-aza-dC）和valproic acid（VPA）预处理PC3-PSMA和LNCaP前列腺癌细胞系5天，随后与177Lu螯合的Vipivotide tetraxetan（50kBq/1mL）共孵育1-24小时，5-aza-dC和VPA显著增加了Vipivotide tetraxetan的细胞摄取[5]。¹⁶¹Tb或¹⁷⁷Lu标记的Vipivotide tetraxetan（0.1-10MBq/mL）处理PSMA阳性的PC-3 PIP肿瘤细胞4小时。¹⁶¹Tb或¹⁷⁷Lu标记的Vipivotide tetraxetan显著降低细胞活力与存活[6]。
在体内，¹⁷⁷Lu标记的Vipivotide tetraxetan（37MBq/只）通过尾静脉单次注射处理携带HepG2肝细胞癌异种移植瘤的BALB/c裸鼠。¹⁷⁷Lu标记的Vipivotide tetraxetan能显著抑制肿瘤生长并延长荷瘤小鼠的生存期[7]。¹⁷⁷Lu标记的Vipivotide tetraxetan（120，160，200MBq/只）通过尾静脉单次注射处理BALB/cAnNRj小鼠。¹⁷⁷Lu标记的Vipivotide tetraxetan能引起小时暂时性的血液毒性（包括白细胞、红细胞和血小板计数的下降），但不会引起死亡[8]。
| Cell experiment [1]: | |
Cell lines | PC-3 PIP (PSMA-positive human prostate cancer cell line) and PC-3 flu (PSMA-negative human prostate cancer cell line) |
Preparation Method | PC-3 PIP and PC-3 flu cells were maintained in RPMI-1640 medium supplemented with 10% fetal calf serum, L-glutamine, and antibiotics at 37°C, 5% CO₂. Cell treatment with ¹⁶¹Tb- or ¹⁷⁷Lu-labeled Vipivotide tetraxetan (0.1-10MBq/mL). |
Reaction Conditions | 0.1-10MBq/mL; 4 hours. |
Applications | ¹⁶¹Tb-labeled Vipivotide tetraxetan significantly and more effectively reduced the viability and survival of PSMA-positive PC-3 PIP tumor cells in an activity concentration-dependent manner compared to ¹⁷⁷Lu-labeled Vipivotide tetraxetan. The effects on PSMA-negative PC-3 flu cells were minimal and comparable for both radioligands. |
| Animal experiment [2]: | |
Animal models | BALB/cAnNRj mice |
Preparation Method | Mice were injected with a single dose of ¹⁷⁷Lu-labeled Vipivotide tetraxetan (at activities of 120, 160, or 200MBq) via the tail vein. Blood samples were collected at multiple time points (4, 13, 17, 21, 25, and 32 days post-injection) for hematological analysis, and animals were sacrificed 32 days post-injection. |
Dosage form | 120, 160, 200MBq per mouse; i.v.; single injection. |
Applications | Administration of ¹⁷⁷Lu-labeled Vipivotide tetraxetan led to transient hematological toxicity, including a significant reduction in white blood cells, red blood cells, and platelets. All blood values returned to normal levels within 32 days, and no radiation-related deaths were observed. |
References: | |
| Cas No. | 1702967-37-0 | SDF | |
| 别名 | PSMA-617 | ||
| Canonical SMILES | O=C(O)[C@H](CCCCNC([C@H](CC1=CC=C2C=CC=CC2=C1)NC([C@H]3CC[C@H](CNC(CN4CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC4)=O)CC3)=O)=O)NC(N[C@H](C(O)=O)CCC(O)=O)=O | ||
| 分子式 | C49H71N9O16 | 分子量 | 1042.14 |
| 溶解度 | DMSO : 125 mg/mL (119.95 mM) | 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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1 mg | 5 mg | 10 mg |
| 1 mM | 959.6 μL | 4.7978 mL | 9.5956 mL |
| 5 mM | 191.9 μL | 959.6 μL | 1.9191 mL |
| 10 mM | 96 μL | 479.8 μL | 959.6 μL |
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