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INH154

Cat No.:V32555 Purity: ≥98%
INH154 (INH-154) is a novel and potent inhibitor for Nek2 and Hec1 with anticancer activity.
INH154
INH154 Chemical Structure CAS No.: 1587705-63-2
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
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Product Description

INH154 (INH-154) is a novel and potent inhibitor for Nek2 and Hec1 with anticancer activity. It inhibits Nek2 and Hec1 with IC50s of 200 nM and 120 nM in Hela and MB468 cells.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
INH154 is particularly successful in treating breast cancers with increased expression of both Hec1 and Nek2. INH154 is the most effective tumor cell growth inhibitor. The IC50 values of INH154 in HeLa and MDA-MB-468 cancer cells were 0.20 and 0.12 μM, respectively. INH154 also suppresses the growth of leukemia, osteosarcoma, and glioblastoma cells [1].
ln Vivo
In a dose-dependent way, tumor growth was markedly slowed in mice treated with INH154 compared to control animals. Tumor proliferation index evaluated by BrdU staining showed a significant reduction in residual tumor under treatment with INH154 when compared to vehicle alone, which is consistent with the tumor growth results. In comparison to tumors treated with a vehicle, INH154-treated tumors exhibited considerably decreased expression levels of Nek2 and Hec1 S165 phosphorylation. However, there was hardly any change between the treatment and control groups when the mice's body weight was assessed during the 6.5-week treatment period. Additionally, when high-dose INH154 (20 mg/kg) was used to treat INH toxicity in normal BALB/c ByJNarl mice, there were no discernible changes in these animal groups' body weight, blood chemistry, or complete blood count (CBC) analysis [1].
References

[1]. Novel small molecules disrupting Hec1/Nek2 interaction ablate tumor progression by triggering Nek2 degradation through a death-trap mechanism. Oncogene. 2015 Mar 5;34(10):1220-30.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H24N4OS
Molecular Weight
392.517163276672
Exact Mass
392.167
CAS #
1587705-63-2
PubChem CID
91669222
Appearance
Light yellow to yellow solid powder
LogP
4.4
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
4
Heavy Atom Count
28
Complexity
509
Defined Atom Stereocenter Count
0
SMILES
S1C(NC(C2C=CN=CC=2)=O)=NC(=C1)C1C(C)=CC(=CC=1C)N1CCCCC1
InChi Key
BBVORAZSFSZSKG-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H24N4OS/c1-15-12-18(26-10-4-3-5-11-26)13-16(2)20(15)19-14-28-22(24-19)25-21(27)17-6-8-23-9-7-17/h6-9,12-14H,3-5,10-11H2,1-2H3,(H,24,25,27)
Chemical Name
N-[4-(2,6-dimethyl-4-piperidin-1-ylphenyl)-1,3-thiazol-2-yl]pyridine-4-carboxamide
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 : ~83.33 mg/mL (~212.29 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 6.25 mg/mL (15.92 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 62.5 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: 2.5 mg/mL (6.37 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 3: 2.5 mg/mL (6.37 mM) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
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.


Solubility in Formulation 4: ≥ 2.08 mg/mL (5.30 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 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 2.5476 mL 12.7382 mL 25.4764 mL
5 mM 0.5095 mL 2.5476 mL 5.0953 mL
10 mM 0.2548 mL 1.2738 mL 2.5476 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:
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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
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  • 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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