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