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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.
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].
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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].
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References |
Molecular Formula |
C22H24N4OS
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Molecular Weight |
392.517163276672
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Exact Mass |
392.167
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CAS # |
1587705-63-2
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PubChem CID |
91669222
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Appearance |
Light yellow to yellow solid powder
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LogP |
4.4
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Hydrogen Bond Donor Count |
1
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Hydrogen Bond Acceptor Count |
5
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Rotatable Bond Count |
4
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Heavy Atom Count |
28
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Complexity |
509
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Defined Atom Stereocenter Count |
0
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SMILES |
S1C(NC(C2C=CN=CC=2)=O)=NC(=C1)C1C(C)=CC(=CC=1C)N1CCCCC1
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InChi Key |
BBVORAZSFSZSKG-UHFFFAOYSA-N
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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)
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Chemical Name |
N-[4-(2,6-dimethyl-4-piperidin-1-ylphenyl)-1,3-thiazol-2-yl]pyridine-4-carboxamide
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~212.29 mM)
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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. View More
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. 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. |
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.
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.