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PNU-159682 carboxylic acid

  CAS No.: 1204819-92-0   Cat No.: BADC-01357 4.5  

PNU-159682 carboxylic acid (compound 53) is a potent ADC cytotoxin encoding a member of the C-type lectin/C-type lectin-like domain (CTL/CTLD) superfamily. PNU-159682 carboxylic acid is involved in protein folding and diverse functions such as cell adhesion, cell signaling, glycoprotein turnover, and roles in inflammation and immune responses.

PNU-159682 carboxylic acid

Structure of 1204819-92-0

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Category
ADC Cytotoxin
Molecular Formula
C31H33NO13
Molecular Weight
627.59
Storage
Store at -20°C

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

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Synonyms
(2S,4S)-2,5,12-trihydroxy-7-methoxy-4-{[(1S,3R,4aS,9S,9aR,10aS)-9-methoxy-1-methyloctahydro-1H-pyrano[4',3':4,5][1,3]oxazolo[2,3-c][1,4]oxazin-3-yl]oxy}-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracene-2-carboxylic acid
IUPAC Name
(2S,4S)-2,5,12-trihydroxy-7-methoxy-4-[[(2S,4R,6S,7S,9R,10S)-10-methoxy-6-methyl-5,8,11-trioxa-1-azatricyclo[7.4.0.02,7]tridecan-4-yl]oxy]-6,11-dioxo-3,4-dihydro-1H-tetracene-2-carboxylic acid
Canonical SMILES
CC1C2C(CC(O1)OC3CC(CC4=C3C(=C5C(=C4O)C(=O)C6=C(C5=O)C(=CC=C6)OC)O)(C(=O)O)O)N7CCOC(C7O2)OC
InChI
InChI=1S/C31H33NO13/c1-12-27-15(32-7-8-42-29(41-3)28(32)45-27)9-18(43-12)44-17-11-31(39,30(37)38)10-14-20(17)26(36)22-21(24(14)34)23(33)13-5-4-6-16(40-2)19(13)25(22)35/h4-6,12,15,17-18,27-29,34,36,39H,7-11H2,1-3H3,(H,37,38)/t12-,15-,17-,18-,27+,28+,29-,31-/m0/s1
InChIKey
QRJDFOACHALIRS-LURYFDOKSA-N
Storage
Store at -20°C

PNU-159682 Carboxylic Acid is a highly potent derivative of the anthracycline family and a notable ADC cytotoxin frequently used as an ADC payload in the development of antibody-drug conjugates. Its mechanism of action involves intercalation into DNA and inhibition of topoisomerase II, which induces double-strand DNA breaks and triggers rapid apoptosis in rapidly dividing tumor cells. The carboxylic acid modification enhances its conjugation compatibility with antibody linkers, providing improved stability and versatility in ADC design.

Within antibody-drug conjugates, PNU-159682 Carboxylic Acid is typically attached to monoclonal antibodies via cleavable or non-cleavable linker chemistries. This ensures that the payload remains inactive in systemic circulation and is selectively released inside tumor cells after internalization and enzymatic processing. The ADC-specific delivery mechanism allows potent cytotoxicity directly at the tumor site, minimizing off-target toxicity and enhancing the therapeutic index. Its extremely high potency makes it effective even at low drug-to-antibody ratios (DARs), which is critical for precision oncology applications.

Applications of PNU-159682 Carboxylic Acid include its use in preclinical and clinical ADC candidates targeting both hematologic malignancies and solid tumors, such as leukemia, lymphoma, breast cancer, and lung cancer. Its chemical structure supports conjugation with various linker technologies, optimizing stability, intracellular release, and overall ADC performance. Researchers leverage PNU-159682 Carboxylic Acid to develop next-generation ADCs with superior antitumor efficacy, tumor selectivity, and reduced systemic side effects.

What is PNU-159682 carboxylic acid?

PNU-159682 carboxylic acid is a highly cytotoxic anthracycline derivative used as a payload in ADCs. It intercalates into DNA and inhibits topoisomerase II, triggering apoptosis, and is compatible with conjugation to antibodies for selective delivery.

7/1/2018

Dear team, how is PNU-159682 carboxylic acid utilized in ADC design?

It is conjugated to antibodies to direct cytotoxic activity toward antigen-expressing cells, ensuring selective cell killing. This approach enhances the therapeutic index while reducing systemic exposure.

25/1/2017

What linker strategies are commonly used for PNU-159682 carboxylic acid?

Cleavable linkers can be used to enable intracellular release upon target cell uptake, while non-cleavable linkers improve systemic stability. Linker selection is critical to optimize efficacy and pharmacokinetic behavior.

7/12/2018

Could you please let me know what safety considerations are important for handling PNU-159682 carboxylic acid?

Due to high cytotoxic potential, laboratory safety protocols must be strictly followed, including PPE, biosafety cabinets, and proper containment. Controlled handling prevents exposure during conjugation and research workflows.

25/5/2016

Good afternoon! What advantages do PNU-159682 carboxylic acid ADCs offer?

These ADCs provide potent and selective cytotoxicity, improving therapeutic precision in preclinical studies. They facilitate evaluation of novel antibody constructs, allowing safer and more targeted drug delivery research.

8/3/2019

— Dr. James Parker, Lead Scientist (USA)

High-purity PNU-159682 carboxylic acid enabled smooth ADC conjugation and in vitro studies.

7/12/2018

— Dr. Patrick O’Neill, ADC Development Specialist (Ireland)

PNU-159682 carboxylic acid supplied by BOC Sciences proved to be of impeccable quality. The detailed COA and consistent results were invaluable for our cytotoxic linker evaluations.

8/3/2019

— Dr. Lars Fischer, Medicinal Chemist (Germany)

Detailed QC and timely delivery of PNU-159682 carboxylic acid ensured smooth project progression.

25/5/2016

— Dr. Anna Peterson, Drug Development Specialist (Sweden)

We tested PNU-159682 carboxylic acid in conjugation with novel linkers, and the results were highly encouraging. BOC Sciences’ material showed stability and activity far exceeding our baseline controls.

7/1/2018

— Dr. William Hayes, Principal Investigator (USA)

Excellent documentation and batch consistency of PNU-159682 carboxylic acid. Critical for cytotoxicity assays.

— Mr. Ethan Clark, Pharmaceutical Scientist (Canada)

For PNU-159682 carboxylic acid, BOC Sciences provided both reliability and speed. The material was shipped under proper storage conditions, ensuring uncompromised quality for our ADC studies.

25/1/2017

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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Historical Records: MA-PEG4-VC-PAB-DMEA-PNU159682 | SG3199 | Mal-PEG2-NHS ester | Cryptophycin 1 | Telomestatin | Mal-PEG2-acid | PNU159682-EDA | MC-VC-PAB-DMEA-PNU159682 | DMEA-PNU-159682 | DBCO-PEG4-VC-PAB-DMEA-PNU159682 | PNU-159682 carboxylic acid
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