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NSC 601980

Cat No.:V57056 Purity: ≥98%
In the yeast screening experiment results of NSC 601980, it showed anti-tumor activity and could effectively inhibit cell proliferation/growth in COLO 205 and HT29 cell lines, with Log GI 50 of -6.6 and -6.9 respectively.
NSC 601980
NSC 601980 Chemical Structure CAS No.: 2070018-27-6
Product category: Others 12
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
50mg
Other Sizes

Other Forms of NSC 601980:

  • NSC 601980 analog
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
In the yeast screening experiment results of NSC 601980, it showed anti-tumor activity and could effectively inhibit cell proliferation/growth in COLO 205 and HT29 cell lines, with Log GI 50 of -6.6 and -6.9 respectively.
NSC 601980 is a synthetic small molecule with antitumor activity. It inhibits cell proliferation in COLO205 (Log GI50 -6.6) and HT29 (Log GI50 -6.9) cancer cell lines in yeast screening experiments.
Biological Activity I Assay Protocols (From Reference)
Targets
26S proteasome and microtubules. NSC 601980 is reported as a 26S proteasome inhibitor that blocks proteasome-mediated protein degradation, leading to protein accumulation and apoptosis in tumor cells. It may also act as a microtubule-disrupting agent, interfering with microtubule assembly.
ln Vitro
NSC 601980 effectively inhibits cell proliferation in COLO 205 and HT29 cell lines with Log GI50 values of -6.6 and -6.9 respectively, demonstrating antitumor potency in yeast screening assays.
ln Vivo
No specific in vivo data reported; however, based on its anti-proliferative activity in vitro, it is suggested to induce tumor growth inhibition in xenograft models. Further in vivo validation studies are needed.
Enzyme Assay
NSC 601980 is dissolved in DMSO to prepare stock solutions. For binding studies, the compound is incubated with purified 26S proteasome or tubulin at concentrations ranging from 0.1-100 uM in assay buffer (50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM ATP) for 30-60 min at 37degC. Proteasome activity is measured using fluorogenic substrates (e.g., Suc-LLVY-AMC). Inhibition of tubulin polymerization can be assessed spectrophotometrically at 340 nm.
Cell Assay
COLO 205 or HT29 cells are seeded in 96-well plates at 5×103 cells/well and treated with NSC 601980 (0.1-100 microM) for 48-72 h. Cell viability is assessed using MTT or CellTiter-Glo assay. GI50 values are calculated by nonlinear regression. Apoptosis induction can be confirmed by Annexin V/PI staining followed by flow cytometry.
Animal Protocol
No in vivo animal study protocols are specifically documented. Based on similar antitumor compounds, a typical regimen might involve intraperitoneal or intravenous administration at doses ranging from 5-50 mg/kg daily or every other day for 2-3 weeks in immunodeficient mice bearing tumor xenografts. Endpoints include tumor volume measurement, body weight monitoring, and terminal histopathology. Researchers should design pilot studies to establish appropriate dosing.
ADME/Pharmacokinetics
Cannot be extracted; information not available. For this compound, no pharmacokinetic data has been published. Investigators are advised to conduct their own PK studies: typical approaches include LC-MS/MS analysis of plasma samples after IV or PO administration to determine key parameters such as half-life (t1/2), clearance (CL), volume of distribution (Vd), and oral bioavailability (F%).
Toxicity/Toxicokinetics
NSC 601980 has not undergone standard toxicity testing. It is intended for research use only. Based on its mechanism as a proteasome inhibitor, potential toxicities may include gastrointestinal and hematologic effects, similar to clinically used proteasome inhibitors, but these have not been formally evaluated for this specific analog.
References
[1]. DTP Datawarehouse Index Results.
Additional Infomation
NSC 601980 is available in high purity (≥95%) for research purposes. The exact IUPAC name is (3-methylquinoxalin-2-yl)-phenyldiazene. Synonyms include 3-methylquinoxalin-2-yl)-phenyldiazene. Molecular formula: C15H12N4; molecular weight: 248.28. It is not approved for clinical use.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H12N4
Molecular Weight
248.28
Exact Mass
248.106
CAS #
2070018-27-6
Related CAS #
NSC 601980 (analog);91757-46-9
PubChem CID
121230984
Appearance
Pink to red solid powder
Density
1.2±0.1 g/cm3
Boiling Point
420.2±45.0 °C at 760 mmHg
Flash Point
207.9±28.7 °C
Vapour Pressure
0.0±1.0 mmHg at 25°C
Index of Refraction
1.658
LogP
3.76
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
2
Heavy Atom Count
19
Complexity
311
Defined Atom Stereocenter Count
0
SMILES
N1C2C(=CC=CC=2)N=C(N=NC2=CC=CC=C2)C=1C
InChi Key
HUXPPDSCOMVLMY-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H12N4/c1-11-15(19-18-12-7-3-2-4-8-12)17-14-10-6-5-9-13(14)16-11/h2-10H,1H3
Chemical Name
(3-methylquinoxalin-2-yl)-phenyldiazene
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: 25 mg/mL (100.69 mM)
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.0277 mL 20.1386 mL 40.2771 mL
5 mM 0.8055 mL 4.0277 mL 8.0554 mL
10 mM 0.4028 mL 2.0139 mL 4.0277 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.

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