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Art. -Nr.: HY-174460

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pCR8

pCR8 is a CR8 prodrug and anticancer agent responsive to H₂O₂. pCR8 achieves selective release of CR8 via boronate ester oxidation mediated by elevated hydrogen peroxide levels at tumor sites, self-assembles into nanoparticles, and degrades cell cycle-related proteins. A synergistic effect is produced when pCR8 is used in combination with immune checkpoint inhibitors. pCR8 can be used for the research of triple-negative breast cancer.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₃₂H₃₆BN₇O₅
Molecular Weight:609.48

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (287 KB)

pCR8 Chemical Structure

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
NIH3T3	IC50	1.552 μM	Cytotoxicity against mouse muscle fibroblast NIH3T3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay. Cytotoxicity against mouse muscle fibroblast NIH3T3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.	40533928
4T1	IC50	0.933 μM	Cytotoxicity against triple-negative breast cancer 4T1 cells assessed as reduction in cell viability incubated for 72 hrs without H₂O₂ by CCK-8 assay. Cytotoxicity against triple-negative breast cancer 4T1 cells assessed as reduction in cell viability incubated for 72 hrs without H₂O₂ by CCK-8 assay.	40533928

In Vitro

pCR8 is an H₂O₂-responsive prodrug that efficiently releases CR8 in H₂O₂-rich conditions, with a 2.5 h half-life for CR8 release in 10 mM H₂O₂, while remaining stable without H₂O₂ stimulation; it also releases CR8 in the presence of 100 μM H₂O₂^[1].
pCR8 (0.04-5 μM; 72 h) has low cytotoxicity to NIH3T3 normal fibroblasts, with an IC₅₀ of 1.552 μM after 72 h incubation^[1].
pCR8 (0.04-5 μM; 72 h) exhibits selective cytotoxicity to 4T1 triple-negative breast cancer cells, with an IC₅₀ of 0.933 μM after 72 h incubation, and its cytotoxicity is significantly enhanced by 400 μM H₂O₂ stimulation^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

NIH3T3 mouse muscle fibroblast cells
Concentration:

0.04-5 μM
Incubation Time:

72 h
Result:

Exhibited reduced cytotoxicity with an IC₅₀ of 1.552 μM.

Cell Cytotoxicity Assay^[1]

Cell Line:

4T1 triple-negative breast cancer cells
Concentration:

0.04-5 μM; 400 μM H₂O₂
Incubation Time:

72 h
Result:

Showed relatively low cytotoxicity with an IC₅₀ of 0.933 μM without H₂O₂.
Demonstrated significantly enhanced cytotoxicity in the presence of 400 μM H₂O₂.

In Vivo

pCR8 (10 mg/kg; i.v.; every 2 days; 8 days) exhibits potent tumor-suppressive activity in 4T1 tumor-bearing BALB/c mice, activates CD8⁺ T cells, and demonstrates enhanced synergistic efficacy when combined with aPD-L1, while maintaining improved safety compared to CR8^[1].

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

Animal Model:

BALB/c (female, 6 weeks old, subcutaneously injected with 5×10⁵ 4T1 cells)^[1]
Dosage:

10 mg/kg (monotherapy); 10 mg/kg (combination with aPD-L1)
Administration:

i.v.; every 2 days; 8 days; i.p. (aPD-L1, every 3 days; 8 days)
Result:

Suppressed tumor growth, with reduced tumor weight and volume compared to the PBS group.
Decreased CCNK and CDK12 expression in tumor tissues relative to the PBS group.
Increased the percentage of CD8⁺ T cells in tumor tissues compared to the PBS group.
Produced the most significant tumor suppression when combined with aPD-L1, with average tumor volume less than 50 mm³ after treatment.
Showed the highest levels of CD8⁺ T cells and GzmB⁺ CD8⁺ T cells in blood, tumor, and spleen tissues when combined with aPD-L1.
Upregulated IL-6, IL-12, IFN-γ, and TNF-α in tumor tissues to the greatest extent when combined with aPD-L1.
Maintained stable body weights, with no significant differences in white blood cell count, red blood cell count, hemoglobin, or platelet count compared to the PBS group.
Showed normal liver and kidney function markers (alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, urea nitrogen, creatinine) with no significant tissue damage in heart, liver, spleen, lung, or kidney.

Chemical Information

Molecular Weight 609.48
Formel C₃₂H₃₆BN₇O₅
SMILES

CC[C@@H](COC(OCC1=CC=C(B(O)O)C=C1)=O)NC2=NC(NCC(C=C3)=CC=C3C4=CC=CC=N4)=C(N=CN5C(C)C)C5=N2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhang N, et al. Self-Assembled Molecular Glue Prodrug System for Enhanced Synergistic Tumor Therapy by Combining CDK12 Protein Degradation and Immunotherapy. ACS applied materials & interfaces. 2025 Jul 02;17(26):37435-37447. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

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100 mg

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