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);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;N-[1,1′-Biphenyl-2-yl]-7-nitro-2,1,3-Benzoxadiazol-4-amine
- CBNumber
- CB92582970
- Molecular Formula
- C18H12N4O3
- Formula Weight
- 332.31
- MOL File
- 413611-93-5.mol
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
Safety
- Hazard Codes
- T
- Risk Statements
- 25-36/37/38
- Safety Statements
- 26-45
- RIDADR
- UN 2811 6.1 / PGIII
- WGK Germany
- 3
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.
N-Bromosuccinimide Price
- Product number
- G3798
- Product name
- 10074-G5
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $120
- Updated
- 2024/03/01
- Product number
- 475957
- Product name
- c-Myc Inhibitor II
- Packaging
- 10mg
- Price
- $126
- Updated
- 2023/06/20
- Product number
- 17408
- Product name
- 10074-G5
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 17408
- Product name
- 10074-G5
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $70
- Updated
- 2024/03/01
- Product number
- G3798
- Product name
- 10074-G5
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $492
- Updated
- 2024/03/01
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 (KD = 4.4 μM), while 10058-F4 interaction site is located within aa residues 402 through 412 (KD = 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
- 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