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PSMA-617 

Cat. No.: HY-117410 Purity: 99.38%
Handling Instructions

PSMA-617 is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM.

For research use only. We do not sell to patients.

PSMA-617 Chemical Structure

PSMA-617 Chemical Structure

CAS No. : 1702967-37-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 1548 In-stock
Estimated Time of Arrival: December 31
1 mg USD 220 In-stock
Estimated Time of Arrival: December 31
5 mg USD 770 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 4750 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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

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 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 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 PSMA-617[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9596 mL 4.7978 mL 9.5956 mL
5 mM 0.1919 mL 0.9596 mL 1.9191 mL
10 mM 0.0960 mL 0.4798 mL 0.9596 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

1042.14

Formula

C₄₉H₇₁N₉O₁₆

CAS No.

1702967-37-0

SMILES

O=C(O)[[email protected]](CCCCNC([[email protected]](CC1=CC=C2C=CC=CC2=C1)NC([[email protected]]3CC[[email protected]](CNC(CN4CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC4)=O)CC3)=O)=O)NC(N[[email protected]](C(O)=O)CCC(O)=O)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PSMA-617
Cat. No.:
HY-117410
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PSMA-617

Cat. No.: HY-117410