2411584-25-1

2411584-25-1 structure
2411584-25-1 structure
  • Name: ERCC1-XPF-IN-1
  • Chemical Name: ERCC1-XPF-IN-1
  • CAS Number: 2411584-25-1
  • Molecular Formula: C28H32ClN5O2
  • Molecular Weight: 506.04
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage DNA/RNA Synthesis
  • Create Date: 2022-07-12 08:04:56
  • Modify Date: 2025-08-26 14:26:26
  • ERCC1-XPF-IN-1 is a potent and high-affinity ERCC1-XPF inhibitor with IC50 value of 0.49 μM. ERCC1-XPF-IN-1 has the capacity to potentiate the cytotoxicity effect of UV radiation and inhibiting DAN repair, by the inhibition of removal of CPDs, and cyclophosphamide toxicity to colorectal cancer cells[1].

Name ERCC1-XPF-IN-1
Description ERCC1-XPF-IN-1 is a potent and high-affinity ERCC1-XPF inhibitor with IC50 value of 0.49 μM. ERCC1-XPF-IN-1 has the capacity to potentiate the cytotoxicity effect of UV radiation and inhibiting DAN repair, by the inhibition of removal of CPDs, and cyclophosphamide toxicity to colorectal cancer cells[1].
Related Catalog
Target

IC50: 0.49 μM (ERCC1-XPF)[1]

In Vitro ERCC1-XPF-IN-1 (compound B7) (2 μM; 0-24 hours) significantly inhibits the removal of CPDs in UV-irradiated HCT-116 cells[1]. ERCC1-XPF-IN-1 (5-20 μM; 72 hours) exhibits approximately 95% of the HCT116 cells survived at 5 μM[1]. ERCC1-XPF-IN-1 (2 and 4 μM; 72 hours) significantly sensitizes HCT 116 cells to cyclophosphamide[1]. Cell Cytotoxicity Assay Cell Line: HCT-116[1] Concentration: 5, 10, 15 and 20 μM Incubation Time: 72 hours Result: Exhibited approximately 95% of the HCT116 cells survived at 5 μM.
In Vivo ERCC1-XPF-IN-1 has a moderate rate of metabolism in human liver microsomes, with log D value of 2.01 at pH 7.4 and an efflux ratio ≥ 43.39[1].
References

[1]. Elmenoufy AH, Gentile F, Jay D, et al. Design, synthesis and in vitro cell-free/cell-based biological evaluations of novel ERCC1-XPF inhibitors targeting DNA repair pathway. Eur J Med Chem. 2020;204:112658.

Molecular Formula C28H32ClN5O2
Molecular Weight 506.04
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