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NSC228155

Alias: NSC228155; NSC-228155; NSC 228155
Cat No.:V2675 Purity: ≥98%
NSC228155 is a novel and potent activator of EGFR, which binds to the sEGFR dimerization domain II and modulate EGFR tyrosine phosphorylation.
NSC228155
NSC228155 Chemical Structure CAS No.: 113104-25-9
Product category: EGFR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

NSC228155 is a novel and potent activator of EGFR, which binds to the sEGFR dimerization domain II and modulate EGFR tyrosine phosphorylation. Previous study found that NSC228155 could dose-dependently inhibit KIX–KID interaction as measured by the split RLuc assay. In living HEK 293T cells, NSC228155 could inhibit CREB-mediated gene transcription with an IC50 of 2.09 μM. NSC228155 also inhibited VP16-CREB-mediated gene transcription with an IC50 of 6.14 μM. Though this was around 3-fold higher than the IC50 of CREB-mediated gene transcription, such results indicated that NSC228155 was not particularly selective in inhibiting KIX–KID interaction inside these living cells.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Through the activity of SOD1, NSC 228155 (100 μM) increases EGFR tyrosine phosphorylation[1]. With IC50 values of 2.09 and 6.14 μM, respectively, NSC 228155 (compound 1) suppresses CREB- and VP16-CREB-mediated gene transcription in vivo HEK 293T cells [2]. In live HEK 293T cells, NSC 228155 is not selective for CREB-mediated gene transcription [2].
ln Vivo
Up to now, there is no animal in vivo data reported.
Animal Protocol


References

[1]. Activation of EGFR by small compounds through coupling the generation of hydrogen peroxide to stable dimerization of Cu/Zn SOD1. Sci Rep. 2016 Feb 17;6:21088.

[2]. Identification, synthesis and evaluation of substituted benzofurazans as inhibitors of CREB-mediated gene transcription. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5371-5.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H6N4O4S
Molecular Weight
290.25
Exact Mass
290.01
CAS #
113104-25-9
Related CAS #
113104-25-9
PubChem CID
313619
Appearance
Light yellow to orange solid powder
Density
1.7±0.1 g/cm3
Boiling Point
627.3±65.0 °C at 760 mmHg
Flash Point
333.2±34.3 °C
Vapour Pressure
0.0±1.8 mmHg at 25°C
Index of Refraction
1.793
LogP
0.07
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
7
Rotatable Bond Count
2
Heavy Atom Count
20
Complexity
369
Defined Atom Stereocenter Count
0
InChi Key
ICCFXXDUYSPKOL-UHFFFAOYSA-N
InChi Code
InChI=1S/C11H6N4O4S/c16-14-6-2-1-3-9(14)20-8-5-4-7(15(17)18)10-11(8)13-19-12-10/h1-6H
Chemical Name
7-nitro-4-(1-oxidopyridin-1-ium-2-yl)sulfanyl-2,1,3-benzoxadiazole
Synonyms
NSC228155; NSC-228155; NSC 228155
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:58 mg/mL (199.8 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: 2 mg/mL (6.89 mM) in 15% Cremophor EL + 85% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 1.6 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.4453 mL 17.2265 mL 34.4531 mL
5 mM 0.6891 mL 3.4453 mL 6.8906 mL
10 mM 0.3445 mL 1.7227 mL 3.4453 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • NSC228155


    Distribution of NBD compounds in breast cancer cells detected with fluorescent microscopy.2016 Feb 17;6:21088.

  • NSC228155


    Detection of ROS in living cells exposed to NBD compounds by fluorescent microscopy.

    NSC228155

    Effects of SOD1 siRNA interference on tyrosine phosphorylation of EGFR, and expression of SOD1 in cancer cells exposed to NBD compounds.

  • NSC228155


    Dimerization of SOD1 in cancer cells exposed to lipophilic NBD compounds, and SOD1 exposed to NBD compoundsin vitro.2016 Feb 17;6:21088.

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