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Vipivotide tetraxetan

  CAS No.: 1702967-37-0   Cat No.: BADC-00818   Purity: >98.0% 4.5  

Vipivotide tetraxetan is a human prostate-specific membrane antigen (PSMA)-targeting ligand that binds to PSMA-expressing tumor cells. Vipivotide tetraxetan could be labeled with 177Lu for imaging and detecting tumors.

Vipivotide tetraxetan

Structure of 1702967-37-0

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Category
ADC Cytotoxin
Molecular Formula
C49H71N9O16
Molecular Weight
1042.14
Target
Prostate-specific Membrane Antigen (PSMA)
Shipping
Room temperature
Shipping
Store at -20 °C

* For research and manufacturing use only. We do not sell to patients.

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Popular Publications Citing BOC Sciences Products
Synonyms
PSMA-617; PSMA 617; PSMA617; Glu-NH-CO-NH-Lys[(2-Nal)-Amc-DOTA]
IUPAC Name
(2S)-2-[[(1S)-1-carboxy-5-[[(2S)-3-naphthalen-2-yl-2-[[4-[[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetyl]amino]methyl]cyclohexanecarbonyl]amino]propanoyl]amino]pentyl]carbamoylamino]pentanedioic acid
Canonical SMILES
C1CC(CCC1CNC(=O)CN2CCN(CCN(CCN(CC2)CC(=O)O)CC(=O)O)CC(=O)O)C(=O)N[C@@H](CC3=CC4=CC=CC=C4C=C3)C(=O)NCCCC[C@@H](C(=O)O)NC(=O)N[C@@H](CCC(=O)O)C(=O)O
InChI
InChI=1S/C49H71N9O16/c59-40(28-55-17-19-56(29-42(62)63)21-23-58(31-44(66)67)24-22-57(20-18-55)30-43(64)65)51-27-32-8-12-35(13-9-32)45(68)52-39(26-33-10-11-34-5-1-2-6-36(34)25-33)46(69)50-16-4-3-7-37(47(70)71)53-49(74)54-38(48(72)73)14-15-41(60)61/h1-2,5-6,10-11,25,32,35,37-39H,3-4,7-9,12-24,26-31H2,(H,50,69)(H,51,59)(H,52,68)(H,60,61)(H,62,63)(H,64,65)(H,66,67)(H,70,71)(H,72,73)(H2,53,54,74)/t32?,35?,37-,38-,39-/m0/s1
InChIKey
JBHPLHATEXGMQR-VLOIPPKDSA-N
Sequence
Glu-NH-CO-NH-Lys[(2-Nal)-Amc-DOTA]
Solubility
DMSO: 125 mg/ml (11995 mm, need ultrasonic)
Appearance
White to off-white solid
Shelf Life
0-4°C for short term (days to weeks), or -20°C for long term (months).
Shipping
Room temperature
Storage
Store at -20 °C
Form
Solid
Biological Activity
Vipivotide tetraxetan (PSMA-617) is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM. IC50 & Target: Ki: 0.37 nM (PSMA)[1] . In Vitro: Vipivotide tetraxetan (PSMA-617) demonstrates high radiolytic stability for at least 72 h. A high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined) and highly efficient internalization into LNCaP cells are demonstrated[1] . 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 177Lulabeled 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] .

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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