产品
编 号:F352483
分子式:C18H12N4O3
分子量:332.31
产品类型
结构图
CAS No: 413611-93-5
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产品详情
生物活性:
10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC50 of 146 μM.
体内研究:
The plasma half-life of 10074-G5 in mice treated with 20 mg/kg i.v. is 37 min, and peak plasma concentration was 58 μM, which is 10-fold higher than peak tumor concentration.
体外研究:
10074-G5 inhibits the growth of Daudi Burkitt's lymphoma cells and disruptes c-Myc/Max dimerization. The IC50 values against Daudi and HL-60 cells are 15.6 and 13.5 μM, respectively. 10074-G5 binds the Myc peptide Myc353-437 with a Kd value of 2.8 μM in the region Arg363-Ile381. 10074-G5 binds in a cavity that is created by a kink (Asp379-Ile381) in the N-terminus of an induced helical domain (Leu370–Arg378).