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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C32H36BN7O5
- 分子量:609.48
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
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 |
体外実験
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 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 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.
体内実験
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.
化学情報
-
分子量 609.48
-
分子式 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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)