PSMA-617
PSMA-617 Basic information
- Product Name:
- PSMA-617
- Synonyms:
-
- PSMA-617
- Vipivotide tetraxetan
- L-Lysine, N2-[[[(1S)-1,3-dicarboxypropyl]amino]carbonyl]-N6-[3-(2-naphthalenyl)-N-[[trans-4-[[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]methyl]cyclohexyl]carbonyl]-L-alanyl]-
- Vipivotide tetraxetan (PSMA-617)
- PSMA617,Vipivotide tetraxetan
- Actinium-225-PSMA-Trillium(BAY3563254)
- (((S)-1-Carboxy-5-((S)-3-(naphthalen-2-yl)-2-((1r,4S)-4-((2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetamido)methyl)cyclohexane-1-carboxamido)propanamido)pentyl)carbamoyl)-L-glutamic acid
- (2S)-2-({[(1S)-1-carboxy-5-[(2S)-3-(naphthalen-2-yl)-2-{[(1s,4s)-4-[(2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetamido)methyl]cyclohexyl]formamido}propanamido]pentyl]carbamoyl
- CAS:
- 1702967-37-0
- MF:
- C49H71N9O16
- MW:
- 1042.14
- Product Categories:
-
- ADC
- Mol File:
- 1702967-37-0.mol
PSMA-617 Chemical Properties
- Boiling point:
- 1371.9±65.0 °C(Predicted)
- Density
- 1.322±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Water:150.0(Max Conc. mg/mL);100.13(Max Conc. mM)
DMSO:125.0(Max Conc. mg/mL);83.43(Max Conc. mM) - form
- Solid
- pka
- 1.83±0.10(Predicted)
- color
- White to off-white
- InChIKey
- JBHPLHATEXGMQR-LFWIOBPJSA-N
- SMILES
- C(O)(=O)[C@H](CCCCNC(=O)[C@H](CC1=CC=C2C(=C1)C=CC=C2)NC([C@@H]1CC[C@@H](CNC(CN2CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC2)=O)CC1)=O)NC(N[C@H](C(O)=O)CCC(O)=O)=O
PSMA-617 Usage And Synthesis
Uses
PSMA-617 has been used in prostate cancer research, and is a promising prostate-specific membrane antigen-targeted theranostic agent.
in vivo
Organ distribution with 68Ga-labeled Vipivotide tetraxetan (PSMA-617) after 1 h (n=3) reveals a high specific uptake in LNCaP tumors and in the kidneys. The high uptake in the kidneys is nearly completely blocked by coinjection of 2 mg of 2-PMPA per kilogram. Other organs such as the liver, lung, and spleen show rather low uptake and no blocking effect, with the exception of the spleen. Tumor-to-background ratios are 7.8 (tumor to blood) and 17.1 (tumor to muscle) at 1 h after injection. As compared with the 68Ga-labeled version, the organ distribution with 177Lu-labeled Vipivotide tetraxetan (PSMA-617) (n=3) show a similar uptake in the LNCaP tumors and in the kidneys. The liver uptake is found to be statistically different. Tumor-to-background ratios 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].
IC 50
Traditional Cytotoxic Agents
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