DC Chemicals · Product datasheet

10074-G5 — Datasheet

CAT. NO. DC10075

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ParameterValue
Chemical Name10074-G5
CAS No.413611-93-5
Synonyms10074-G5;10074G5;4-nitro-N-(2-phenylphenyl)-2,1,3-benzoxadiazol-7-amine;Biphenyl-2-yl-(7-nitrobenzo[1,2,5]oxadiazol-4-yl)amine;N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-amine;N-[1,1′-Biphenyl-2-yl]-7-nitro-2,1,3-Benzoxadiazol-4-amine
FormulaC18H12N4O3
M.Wt332.313
SMILESO=[N+]([O-])C1=CC=C(NC2=CC=CC=C2C3=CC=CC=C3)C4=NON=C41
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC50 of 146 μM.

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[1]. 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)[3].

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[1].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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