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编 号:F741285
分子式:C15H13Cl2NO3
分子量:326.17
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
ERCC1-XPF-IN-2 is a potent ERCC1-XPF endonuclease inhibitor with an IC50 value of 0.6 μM. ERCC1-XPF-IN-2 shows activity in nucleotide excision repair, cisplatin enhancement and γH2AX assays.

体外研究:
ERCC1-XPF-IN-2 (compound 13) (0-100 μM) shows FEN-1 and DNase I activity with IC50s of >100, >100 μM, respectively.ERCC1-XPF-IN-2 slow binding kinetics with an Kd value of ~30 μM.ERCC1-XPF-IN-2 shows not toxic to Hep-G2 cells at 10 μM and relatively short mouse and human microsomal half-lives with t1/2 value of 23 min and 28 min for mouse and human, respectively.ERCC1-XPF-IN-2 (0-60 μM; 24 h) shows inhibition of nucleotide excision repair (NER) with an IC50 value of 15.6 μM in A375 cells.ERCC1-XPF-IN-2 (0-60 μM) increases the cisplatin activity with no toxicity.ERCC1-XPF-IN-2 (10 μM; 6h) causes a delay in DNA repair by a right shift towards higher numbers of γH2AX foci per cell.
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