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

ChemicalBook > CAS DataBase List > N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine

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

Product Name: N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine
CAS No.: 413611-93-5
Chemical Name: N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine
Synonyms: 10074-g;10074-G5;10074G5;10074 G5;c-Myc Inhibitor II;10074-G5 >=98% (HPLC);10074-G5, 10 mM in DMSO;c-Myc Inhibitor II - CAS 413611-93-5 - Calbiochem;N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine;Biphenyl-2-yl-(7-nitrobenzo[1,2,5]oxadiazol-4-yl)amine;N-(2-Biphenylyl)-4-amino-7-nitrobenzo[c][1,2,5]oxadiazole
CBNumber: CB92582970
Molecular Formula: C18H12N4O3
Formula Weight: 332.31
MOL File: 413611-93-5.mol

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N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine Property

Boiling point:: 538.6±60.0 °C(Predicted)
Density: 1.408±0.06 g/cm3(Predicted)
storage temp.: room temp
solubility: DMSO: >10mg/mL
pka: -2.06±0.50(Predicted)
form: powder
color: red

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Safety

Hazard Codes: T
Risk Statements: 25-36/37/38
Safety Statements: 26-45
RIDADR: UN 2811 6.1 / PGIII
WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: G3798
Product name: 10074-G5
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $120
Updated: 2024/03/01

Sigma-Aldrich

Product number: 475957
Product name: c-Myc Inhibitor II
Packaging: 10mg
Price: $126
Updated: 2023/06/20

Cayman Chemical

Product number: 17408
Product name: 10074-G5
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 17408
Product name: 10074-G5
Purity: ≥98%
Packaging: 5mg
Price: $70
Updated: 2024/03/01

Sigma-Aldrich

Product number: G3798
Product name: 10074-G5
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $492
Updated: 2024/03/01

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N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine Chemical Properties,Usage,Production

Uses

N-[1,1''-Biphenyl]-2-yl-7-nitro-2,1,3-benzoxadiazol-4-amine is a c-Myc inhibitor that suppresses its transcriptional activity.c-Myc is an oncoprotein often found overexpressed in various tumors.

General Description

A cell-permeable benzoxadiazole compound that is shown to preferentially disrupt the interactions of c-Myc-Max, Mad1-Max, and Myf5-HEB, over those of 31 other pairs of HLH-, ZIP-, and HLH-ZIP-containing proteins. Similarly to 10058-F4 (Cat. No. 475956), 10074-G5 is shown to selectively inhibit the c-Myc-dependent growth of rat fibroblast cell line TGR1 and effectively suppress c-Myc-dependent transcription activity. Binding studies using various mutated and truncated c-Myc constructs reveal that 10074-G5 targets c-Myc helix-1 region between aa 363 and 381 (K_D = 4.4 μM), while 10058-F4 interaction site is located within aa residues 402 through 412 (K_D = 13 μM).

Biological Activity

10074-g5 is a c-myc inhibitor [1].c-myc is a bhlh-zip transcription factor involved in cell cycle progression, cellular growth and metabolism, differentiation, and apoptosis. overexpression of c-myc has been identified in numerous cancers, including prostate, pancreatic, lung, breast, and colon cancers, b-cell lymphoma, and leukemias. alterations in c-myc have been associated with cancer aggressiveness and poor treatment prognosis. inhibition of c-myc is an attractive pharmacological approach in the development of new anticancer treatments. inactivation of c-myc rapidly results in cell-cycle arrest, apoptosis, tumor vascular degeneration, redifferentiation of tumor cells, and ultimately tumor regression [1].the ic50 values of 10074-g5 against daudi cells and hl-60 cells were 15.6 ± 1.5 μm and 13.5 ± 2.1 μm, respectively. 10074-g5 (10 μm) inhibited c-myc/max dimerization and decreased total c-myc protein expression. in c.b-17 scid mice bearing daudi xenografts, treatment with 10074-g5, (20 mg/kg i.v., for 10 consecutive days) significantly inhibited tumor growth with no effects on body weight.

Biochem/physiol Actions

10074-G5 is a c-Myc/Max interaction inhibitor. The c-Myc oncoprotein and its partner Max are intrinsically disordered (ID) monomers that undergo coupled folding and binding upon heterodimerization. 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. 10074-G5 (2.8 microM) is slightly more potent that 10058-F4 (5.2 microM). It was discovered that 10074-G5 binds to a different specific binding site (region) of C-Myc than 10054-F4. Thus, the compound may become desirable for probing different interactions.

References

[1] clausen d m, guo j, parise r a, 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]. journal of pharmacology and experimental therapeutics, 2010, 335(3): 715-727.

N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine manufacturers

Career Henan Chemical Co

Product: N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine 413611-93-5
Price: US $1.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 20kg
Release date: 2019-12-23

413611-93-5, N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMineRelated Search:

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

10074-G5

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

N-[1,1′-Biphenyl-2-yl]-7-nitro-2,1,3-Benzoxadiazol-4-amine

c-Myc Inhibitor II

c-Myc Inhibitor II - CAS 413611-93-5 - Calbiochem

10074G5;10074 G5

10074-g

2,1,3-Benzoxadiazol-4-amine, N-[1,1'-biphenyl]-2-yl-7-nitro-

10074-G5 >=98% (HPLC)

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

10074G5,Inhibitor,10074 G5,10074-G-5,10074-G5,c-Myc,Autophagy,inhibit,Myc

N-(2-Biphenylyl)-4-amino-7-nitrobenzo[c][1,2,5]oxadiazole

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

10074-G5, 10 mM in DMSO

413611-93-5