1. Antibody-drug Conjugate/ADC Related Immunology/Inflammation
  2. Radionuclide-Drug Conjugates (RDCs) PSMA
  3. PDI2

PDI2 (PSMA-DOTA-PEI2) is a prostate-specific membrane antigen (PSMA) ligand that acts as a tumor retention agent, renal uptake reducer, imaging agent and antitumor agent, applicable in SPECT diagnostic imaging and radiotheranostics. PDI2 specifically binds to PSMA on prostate cancer cells, enters cells via clathrin-dependent endocytosis, and exhibits higher tumor retention rate and lower renal uptake level. PDI2 is applicable in research related to prostate cancer and castration-resistant metastatic prostate cancer.

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PDI2

PDI2 Chemical Structure

CAS No. : 3110124-60-9

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Description

PDI2 (PSMA-DOTA-PEI2) is a prostate-specific membrane antigen (PSMA) ligand that acts as a tumor retention agent, renal uptake reducer, imaging agent and antitumor agent, applicable in SPECT diagnostic imaging and radiotheranostics. PDI2 specifically binds to PSMA on prostate cancer cells, enters cells via clathrin-dependent endocytosis, and exhibits higher tumor retention rate and lower renal uptake level. PDI2 is applicable in research related to prostate cancer and castration-resistant metastatic prostate cancer[1].

In Vitro

[111In]In-PDI2 (0.195-50 nM; incubated on ice for 2 h) binds specifically to PSMA on LNCaP cells, with a Kd value of 22.8 nM[1].
[111In]In-PDI2 (37 kBq; incubated on ice for 2 h, incubated at 37°C for 0-4 h) shows an internalization rate of 38.9% in LNCaP cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PDI2 (111 kBq; i.v.; single dose) exhibits high and persistent tumor uptake in the PSMA-positive LNCaP prostate cancer xenograft model, along with a favorable tumor-to-kidney radioactivity ratio[1].
PDI2 (5-10 kBq; i.v.; single dose) effectively inhibits the growth of PSMA-positive LNCaP prostate cancer xenografts with no obvious toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nu/nu (male, 5-6 weeks old)[1]
Dosage: 111 kBq
Administration: i.v.; single dose
Result: Measured 20.74% ID/g tumor accumulation at 4-h postinjection; measured 25.47% ID/g tumor accumulation at 24-h postinjection; measured 13.54% ID/g tumor accumulation at 96-h postinjection; measured 52.31% ID/g renal uptake at 4-h postinjection; measured 4.85% ID/g renal uptake at 24-h postinjection; achieved 7.3 tumor-to-kidney radioactivity ratio.
Molecular Weight

1271.41

Formula

C59H90N12O19

CAS No.
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PDI2
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HY-P11591
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