10074-G5
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 530576

CAS#: 413611-93-5

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.


Chemical Structure

img
10074-G5
CAS# 413611-93-5

Theoretical Analysis

MedKoo Cat#: 530576
Name: 10074-G5
CAS#: 413611-93-5
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

Price and Availability

Size Price Availability Quantity
100.0mg USD 850.0 2 Weeks
200.0mg USD 1250.0 2 Weeks
500.0mg USD 2150.0 2 Weeks
1.0g USD 2950.0 2 Weeks
2.0g USD 5250.0 2 Weeks
5.0g USD 7850.0 2 Weeks
Bulk inquiry

Synonym: 10074-G5; 10074G5; 10074 G5;

IUPAC/Chemical Name: N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine

InChi Key: KMJPYSQOCBYMCF-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: O=[N+]([O-])C1=CC=C(C2=NON=C21)NC3=CC=CC=C3C4=CC=CC=C4

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

Biological target: 10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC50 of 146 μM.
In vitro activity: As shown in Fig. 2A, exposure of MDA-MB-231 cells with 10074-G5 at 10 μM, 25 μM and 50 μM decreased the expression of PC mRNA to 70%, 30% and 20%, respectively. Consistent with mRNA level, 10074-G5 at 10 μM minimally affected expression of PC expression at the protein level while at concentrations of 25 μM and 50 μM suppressed expression of PC protein by 80–90% (Fig. 2B). In contrast, 10074-G5 did not affect the expression of both PC mRNA and PC protein in MCF-7 cells (Fig. 2C and D). The lack of inhibitory effect of 10074-G5 on PC expression in MCF-7 cells was likely caused by lowered expression level of endogenous c-Myc. While inhibition of c-Myc-regulation of PC expression with 10 μM and 25 μM 10074-G5 did not affect growth of MDA-MB-231 cells, treatment of cells with 50 μM 10074-G5 resulted in 25% and 40% decrease in cell growth at days 2 and 3, respectively (Fig. 2E). Reference: Biochim Biophys Acta Mol Basis Dis. 2020 Mar 1;1866(3):165656. https://pubmed.ncbi.nlm.nih.gov/31874204/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.0 113.66
DMSO:PBS (pH 7.2) (1:4) 0.2 0.6
DMF 20.0 59.82
Ethanol 6.0 17.95

Preparing Stock Solutions

The following data is based on the product molecular weight 334.335 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Lao-On U, Rojvirat P, Chansongkrow P, Phannasil P, Siritutsoontorn S, Charoensawan V, Jitrapakdee S. c-Myc directly targets an over-expression of pyruvate carboxylase in highly invasive breast cancer. Biochim Biophys Acta Mol Basis Dis. 2020 Mar 1;1866(3):165656. doi: 10.1016/j.bbadis.2019.165656. Epub 2019 Dec 23. PMID: 31874204. 2. Aksoz M, Albayrak E, Aslan GS, Turan RD, Alyazici LY, Siyah P, Tuysuz EC, Canikyan S, Yucel D, Meric N, Gulbas Z, Sahin F, Kocabas F. c-Myc Inhibitor 10074-G5 Induces Murine and Human Hematopoietic Stem and Progenitor Cell Expansion and HDR Modulator Rad51 Expression. Curr Cancer Drug Targets. 2019;19(6):479-494. doi: 10.2174/1568009618666180905100608. PMID: 30182856.
In vitro protocol: 1. Lao-On U, Rojvirat P, Chansongkrow P, Phannasil P, Siritutsoontorn S, Charoensawan V, Jitrapakdee S. c-Myc directly targets an over-expression of pyruvate carboxylase in highly invasive breast cancer. Biochim Biophys Acta Mol Basis Dis. 2020 Mar 1;1866(3):165656. doi: 10.1016/j.bbadis.2019.165656. Epub 2019 Dec 23. PMID: 31874204. 2. Aksoz M, Albayrak E, Aslan GS, Turan RD, Alyazici LY, Siyah P, Tuysuz EC, Canikyan S, Yucel D, Meric N, Gulbas Z, Sahin F, Kocabas F. c-Myc Inhibitor 10074-G5 Induces Murine and Human Hematopoietic Stem and Progenitor Cell Expansion and HDR Modulator Rad51 Expression. Curr Cancer Drug Targets. 2019;19(6):479-494. doi: 10.2174/1568009618666180905100608. PMID: 30182856.
In vivo protocol: TBD

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

10074-G5

100.0mg / USD 850.0


Additional Information

The c-Myc oncoprotein and its partner Max are intrinsically disordered (ID) monomers that undergo coupled folding and binding upon heterodimerization.