| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
KIF15-IN-1 targets kinesin family member 15 (Kif15), a mitotic kinesin that plays a critical role in spindle assembly during cell division. Kif15 acts redundantly with KIF11 (Eg5) to maintain bipolar spindle formation. By inhibiting Kif15, the compound disrupts mitosis, leading to cell cycle arrest and cell death. Its synergistic effect with Eg5 inhibitors makes it a valuable tool for studying mitosis and for developing combination cancer therapies.
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| ln Vitro |
Compound 10, or Kif15-IN-1, is a multiplex of the mitotic kinesin Hs Kif15 and may be effective in inhibiting the growth of cells in conditions including cancer, ischemia, heart hypertrophy, and immunological activation [1].
In vitro, KIF15-IN-1 inhibits cellular proliferation in various tumor cell lines. It is a potent Kif15 inhibitor. It can be used to study gastric cancer. Its effects on cell cycle and proliferation can be assessed in various cancer cell lines. It is a valuable tool for studying the role of Kif15 in mitosis and cancer. Its synergistic effects with Eg5 inhibitors can be studied in combination assays. |
| ln Vivo |
In vivo, KIF15-IN-1 can be used to study gastric cancer and other cell proliferative diseases. By inhibiting Kif15, it can disrupt tumor growth. Its potential anticancer activity is being evaluated in preclinical studies. Its ability to synergize with Eg5 inhibitors makes it a promising candidate for combination therapy. Further studies are needed to evaluate its in vivo efficacy and safety.
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| Enzyme Assay |
The in vitro kinase assay for KIF15-IN-1 involves measuring its inhibition of Kif15 ATPase activity. Recombinant Kif15 is incubated with varying concentrations of KIF15-IN-1 (0.1-1000 nM) and a microtubule substrate. The ATPase activity is measured using a malachite green phosphate detection assay or a coupled enzyme assay. IC50 values are calculated from dose-response curves. Cell-based assays measure the inhibition of cellular proliferation in tumor cell lines.
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| Cell Assay |
In vitro cellular assays for KIF15-IN-1 use cancer cell lines, such as gastric cancer cells. Cells are cultured in appropriate media and treated with the compound at concentrations of 0.1-1000 nM for 24-72 hours. Cell viability is assessed using MTT or CCK-8 assays. Cell cycle analysis is performed by flow cytometry. Apoptosis is evaluated using caspase-3/7 activity assays and Annexin V staining. The compound's synergistic effects with Eg5 inhibitors are assessed by combination index analysis.
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| Animal Protocol |
In vivo animal studies for KIF15-IN-1 involve mouse xenograft models using human cancer cell lines, such as gastric cancer cells. Tumor-bearing mice are treated with the compound via oral gavage or intraperitoneal injection at doses of 1-50 mg/kg. Tumor volume is measured regularly. The compound's effect on tumor growth is assessed, both as a single agent and in combination with Eg5 inhibitors. Pharmacodynamic studies measure Kif15 inhibition and downstream signaling in tumor tissues.
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| ADME/Pharmacokinetics |
KIF15-IN-1 is a small molecule with good cell permeability. It has a molecular weight of approximately 430.48 and a molecular formula of C20H22N4O5S. It is soluble in DMSO and should be stored at -20°C for long-term preservation as a powder and at -80°C in solvent. Its pharmacokinetic properties, including oral bioavailability, half-life, and tissue distribution, are not extensively reported in the available literature and would need to be characterized for therapeutic applications.
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| References | |
| Additional Infomation |
KIF15-IN-1 is a Kif15 inhibitor with the CAS number 672926-32-8. It has antiproliferative activity and potential anticancer activity. It pairs with Eg5 inhibitors synergistically to reduce cancer cell growth. The compound is a research tool for studying mitosis and cancer, and it is not for human therapeutic use.
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| Molecular Formula |
C20H22N4O5S
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|---|---|
| Molecular Weight |
430.48
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| Exact Mass |
430.131
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| CAS # |
672926-32-8
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| PubChem CID |
60076300
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.619
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| LogP |
3.73
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
703
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCOC(=O)C1=C(N=C(S1)NC(=O)[C@H](C(C)C)N2C(=O)C3=CC=CC=C3NC2=O)C
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| InChi Key |
CTQQKICGMSZCJL-AWEZNQCLSA-N
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| InChi Code |
InChI=1S/C20H22N4O5S/c1-5-29-18(27)15-11(4)21-19(30-15)23-16(25)14(10(2)3)24-17(26)12-8-6-7-9-13(12)22-20(24)28/h6-10,14H,5H2,1-4H3,(H,22,28)(H,21,23,25)/t14-/m0/s1
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| Chemical Name |
ethyl 2-[[(2S)-2-(2,4-dioxo-1H-quinazolin-3-yl)-3-methylbutanoyl]amino]-4-methyl-1,3-thiazole-5-carboxylate
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| Synonyms |
KIF15-IN1; KIF15IN-1; KIF15-IN-1
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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 : ≥ 100 mg/mL (~232.30 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.81 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 25.0 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 (5.81 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 25.0 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 | 2.3230 mL | 11.6149 mL | 23.2299 mL | |
| 5 mM | 0.4646 mL | 2.3230 mL | 4.6460 mL | |
| 10 mM | 0.2323 mL | 1.1615 mL | 2.3230 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.
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