10074-G5


Catalog No. size PriceQuantity
M6589-2 2mg solid $107
M6589-10 10mg solid $452

Description

10074-G5 is a c-Myc/Max interaction inhibitor. 10074-G5, similarly to 10058-F4 (#F3680), specifically inhibits this interaction by binding to c-Myc, thus preventing C-Myc specific DNA binding and target genes regulation.

Product information

CAS Number: 413611-93-5

Molecular Weight: 332.31

Formula: C18H12N4O3

Synonym:

CHEMBL2312756

MLS006012602

Oprea1_158245

SCHEMBL2689577

DTXSID60385481

HMS3743K15

BCP09223

EX-A4226

KS-00000UC6

ZINC3879010

BDBM50423921

s8426

CCG-267830

CS-6372

NCGC00346825-01

AK687962

BS-16819

Chemical Name: Biphenyl-2-yl-(7-nitrobenzo[1,2,5]oxadiazol-4-yl)amine

Smiles: [O-][N+](=O)C1=CC=C(NC2=CC=CC=C2C2C=CC=CC=2)C2=NON=C12

InChiKey: KMJPYSQOCBYMCF-UHFFFAOYSA-N

InChi: InChI=1S/C18H12N4O3/c23-22(24)16-11-10-15(17-18(16)21-25-20-17)19-14-9-5-4-8-13(14)12-6-2-1-3-7-12/h1-11,19H

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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 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).

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.

References:

  1. Clausen DM, et al. In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization. J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.
  2. Yap JL, et al. Pharmacophore identification of c-Myc inhibitor 10074-G5. Bioorg Med Chem Lett. 2013 Jan 1;23(1):370-4.

Products are for research use only. Not for human use.

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