yingweiwo

10074-A4

Alias: 10074-A4 10074A4 10074 A4
Cat No.:V7206 Purity: ≥98%
10074-A4 is a c-Myc inhibitor that can bind to c-Myc370-409 at different positions in the peptide chain.
10074-A4
10074-A4 Chemical Structure CAS No.: 312631-87-1
Product category: New1
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
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text

 

  • Business Relationship with 5000+ Clients Globally
  • Major Universities, Research Institutions, Biotech & Pharma
  • Citations by Top Journals: Nature, Cell, Science, etc.
Top Publications Citing lnvivochem Products
Product Description
10074-A4 is a c-Myc inhibitor that can bind to c-Myc370-409 at different positions in the peptide chain. 10074-A4 has anti-cancer effects.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
10074-A4 has 15.1 μM IC50 inhibitory action against HL-60 cells[1]. In HL-60 cells, 10074-A4 (25-50 μM; 24 hours) dose-dependently stops the cell cycle in the S phase. The c-Myc target genes CDK4 and CCND2 had their mRNA levels inhibited by 10074-A4 [1]. It is possible to characterize 10074-A4's binding behavior to c-Myc370-409 as a "ligand cloud" because it can bind to the peptide chain at several locations. The c-Myc370-409 peptide's structure is still dynamic in its bound state. Different locations throughout the c-Myc370-409 chain bind to the 10074-A4 ligand with varying intensities [2].
Cell Assay
Cell viability assay [1]
Cell Types: HL-60 Cell
Tested Concentrations: 25 μM, 50 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: The cell cycle was arrested in S phase.
References

[1]. Structure-based Inhibitor Design for the Intrinsically Disordered Protein c-Myc. Sci Rep. 2016 Mar 2;6:22298.

[2]. Ligand clouds around protein clouds: a scenario of ligand binding with intrinsically disordered proteins. PLoS Comput Biol. 2013;9(10):e1003249.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H14CL2N2O3S
Molecular Weight
409.28
Exact Mass
408.01
CAS #
312631-87-1
PubChem CID
2836204
Appearance
White to off-white solid powder
LogP
4.095
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
4
Heavy Atom Count
26
Complexity
555
Defined Atom Stereocenter Count
0
InChi Key
SCNHANGMZXFWOH-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H14Cl2N2O3S/c19-10-1-3-15-13(5-10)14-6-11(20)2-4-16(14)21(15)7-12(23)8-22-17(24)9-26-18(22)25/h1-6,12,23H,7-9H2
Chemical Name
3-[3-(3,6-dichlorocarbazol-9-yl)-2-hydroxypropyl]-1,3-thiazolidine-2,4-dione
Synonyms
10074-A4 10074A4 10074 A4
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

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
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 : ~125 mg/mL (~305.41 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (5.08 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 20.8 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 2.4433 mL 12.2166 mL 24.4332 mL
5 mM 0.4887 mL 2.4433 mL 4.8866 mL
10 mM 0.2443 mL 1.2217 mL 2.4433 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.
/

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.)
+
+
+

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
  • Representative conformations of holo c-Myc370–409/10074-A4 complex computed from explicit solvent simulations. Backbone-RMSD clustering with a cutoff of 2.0 Å of all the conformations was performed. Representative c-Myc370–409 structures (from blue at the N-terminal to red at the C-terminal) for the first eight clustering groups were displayed in cartoon and 10074-A4 structures were depicted as black sticks. The fractional cluster populations are: A 14.3%, B 13.9%, C 13.7%, D 10.4%, E 7.5%, F 6.9%, G 5.4%, H 5.2%.[2]. Fan Jin, et al. Ligand clouds around protein clouds: a scenario of ligand binding with intrinsically disordered proteins. PLoS Comput Biol. 2013;9(10):e1003249.
  • Binding specificity of 10074-A4 with c-Myc370–409. The binding-time percentage was computed for each residue by counting the frames with ΔSASA larger than 10 Å2. Continuous binding of less than 10 ns was ignored.[2]. Fan Jin, et al. Ligand clouds around protein clouds: a scenario of ligand binding with intrinsically disordered proteins. PLoS Comput Biol. 2013;9(10):e1003249.
  • Interactions between 10074-A4 and the c-Myc370–409 peptide. A Lennard-Jones potential. B Electrostatic potential. C Time percentage of hydrogen bonds.[2]. Fan Jin, et al. Ligand clouds around protein clouds: a scenario of ligand binding with intrinsically disordered proteins. PLoS Comput Biol. 2013;9(10):e1003249.
Contact Us