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

10074-G5

10074G5

4-nitro-N-(2-phenylphenyl)-2,1,3-benzoxadiazol-7-amine

N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-amine

SMR004704145

HY-100996

10074-G5, &gt

=98% (HPLC)

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: ≥12 months 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.

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed