10074-G5


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

Description

Cas:413611-93-5

Product Information

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.

 

Chemical Formula: C18H14N4O3

 

Exact Mass: 334.335

 

Molecular Weight: 334.335

 

Elemental Analysis: C, 64.67; H, 4.22; N, 16.76; O, 14.36

 

Synonym: 

 

10074-G5

10074G5

CHEMBL2312756

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

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

Oprea1_158245

MLS006012602

SCHEMBL2689577

DTXSID60385481

HMS3743K15

BCP09223

EX-A4226

KS-00000UC6

ZINC3879010

BDBM50423921

s8426

CCG-267830

CS-6372

NCGC00346825-01

AK687962

BS-16819

SMR004704145

HY-100996

10074-G5, >=98% (HPLC)

 

Chemical Name:

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

 

InChi Key:

PSWROULKDNSAAU-UHFFFAOYSA-N

 

InChi Code:

InChI=1S/C18H14N4O3/c23-22(24)18-11-10-16(17-12-19-25-21(17)18)20-15-9-5-4-8-14(15)13-6-2-1-3-7-13/h1-12,19-20H

 

Smiles Code:

O=[N+](C1=CC=C(NC2=CC=CC=C2C3=CC=CC=C3)C4=CNON41)[O-]

 

 

Technical Data:

 

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

 

  1. 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

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

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