ERCC1-XPF-IN-1 

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].

IC₅₀: 0.49 μM (ERCC1-XPF)^[1]

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].

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

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].

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

506.04

C₂₈H₃₂ClN₅O₂

2411584-25-1

Solid

Orange to reddish brown

OC1=CC2=C(NC3=CC=C(O)C(CN4CCN(CCN(C)C)CC4)=C3)C5=CC=C(Cl)C=C5N=C2C=C1

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]