PNU-159682

PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.

Product Specifications

CAS Number

[202350-68-3]

UNSPSC

12352203

Hazard Statement

H302, H315, H319, H335

Target

ADC Payload; Topoisomerase

Type

ADC Related

Related Pathways

Antibody-drug Conjugate/ADC Related; Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pnu-159682.html

Purity

98.57

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

COC1=C(C(C(C(O)=C([C@@H](O[C@H]2C[C@H]3[C@H](O[C@H]4N3CCO[C@@H]4OC)[C@H](C)O2)C[C@@](C(CO)=O)(O)C5)C5=C6O)=C6C7=O)=O)C7=CC=C1

Molecular Formula

C32H35NO13

Molecular Weight

641.62

Precautions

H302, H315, H319, H335

References & Citations

[1]Quintieri L, et al. Formation and antitumor activity of PNU-159682, a major metabolite of nemorubicin in human liver microsomes. Clin Cancer Res. 2005 Feb 15;11 (4) :1608-17.|[2]Cazzamalli S, et al. Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma. Mol Cancer Ther. 2016 Dec;15 (12) :2926-2935.|[3]Pengxuan Zhao, et al. Recent advances of antibody drug conjugates for clinical applications. Acta Pharm Sin B. 2020 Sep;10 (9) :1589-1600.|[4]Joanne Lundy, Interim data: Phase I/IIa study of EGFR-targeted EDV nanocells carrying cytotoxic drug PNU-159682 (E-EDV-D682) with immunomodulatory adjuvant EDVs carrying α-galactosyl ceramide (EDV-GC) in patients with recurrent, metastatic pancreatic cancer. GASTROINTESTINAL CANCER—GASTROESOPHAGEAL, PANCREATIC, AND HEPATOBILIARY