10074-G5,413611-93-5

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10074-G5

CAS No. : 413611-93-5

MCE 国际站：10074-G5

产品活性：10074-G5是c-Myc-Max二聚化抑制剂，IC₅₀值为146 μM。

研究领域：Apoptosis  |  Autophagy

作用靶点：c-Myc  |  Autophagy

In Vitro: 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 K_d 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).

In Vivo: 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.

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