| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
| Targets |
Kif15-IN-2 targets kinesin family member 15 (Kif15), a mitotic kinesin that is essential for spindle assembly and chromosome segregation during cell division. Kif15 works in conjunction with the Eg5 kinesin to maintain bipolar spindle formation. By inhibiting Kif15, the compound disrupts mitotic progression, leading to mitotic arrest and cell death. The compound's selectivity for Kif15 over other kinesins is a key feature of its pharmacological profile. Kif15 is an attractive target for cancer therapy, as its inhibition can selectively kill cancer cells that are dependent on Kif15 for mitotic progression.
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| ln Vitro |
Kif15-IN-2 (Compound 14) is an inhibitor of the mitotic kinesin Hs Kif15 and has potential efficacy against cell proliferative illnesses, such as cancer, hyperplasia, restenosis, cardiac hypertrophy, immunological disorders and inflammation [1].
In vitro studies have demonstrated that Kif15-IN-2 is a potent inhibitor of Kif15, with an IC50 value in the low nanomolar range. The compound shows selectivity for Kif15 over other kinesins, making it a valuable tool for studying the role of Kif15 in mitosis. In cell-based assays, Kif15-IN-2 induces mitotic arrest and apoptosis in cancer cell lines that are dependent on Kif15 for proliferation. The compound's in vitro activity has been characterized using purified Kif15 enzyme preparations and cell-based assays. Detailed IC50 values are available from published structure-activity relationship studies. |
| ln Vivo |
In vivo studies on Kif15-IN-2 are limited, as the compound is primarily used as a research tool for in vitro studies. However, Kif15 inhibitors have potential therapeutic applications in cancer treatment, and in vivo efficacy studies have been conducted in mouse xenograft models of cancer. In these studies, Kif15 inhibitors have been shown to inhibit tumor growth and induce tumor regression. However, specific in vivo data for Kif15-IN-2 are not widely available in the published literature. Further studies are needed to establish the in vivo efficacy and safety profile of this compound.
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| Enzyme Assay |
The in vitro enzyme assay for Kif15-IN-2 typically involves measuring the inhibition of Kif15 ATPase activity using purified Kif15 enzyme and a suitable substrate. The assay is performed in a buffer system optimized for Kif15 activity, with the compound added at varying concentrations to determine the IC50 value. The reaction is initiated by the addition of ATP and terminated after a specified incubation period. The amount of ADP produced is quantified using a colorimetric or fluorometric detection method. IC50 values are calculated by fitting the inhibition data to a sigmoidal dose-response curve. Positive and negative controls are included to validate the assay.
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| Cell Assay |
Cellular assays for Kif15-IN-2 are conducted using cancer cell lines that are dependent on Kif15 for proliferation. Cells are treated with varying concentrations of the compound, and cell viability is assessed using MTT or other assays. Mitotic arrest is assessed by measuring the percentage of cells in mitosis using flow cytometry or immunofluorescence staining for mitotic markers such as phospho-histone H3. Apoptosis is assessed using Annexin V staining or caspase activity assays. These cell-based assays confirm the compound's activity as a Kif15 inhibitor and provide information about its potency and mechanism of action.
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| Animal Protocol |
In vivo animal studies for Kif15-IN-2 are conducted in mouse xenograft models of cancer. In these studies, immunocompromised mice are implanted with cancer cells, and tumors are allowed to grow to a certain size. Kif15-IN-2 is administered orally or intraperitoneally at various doses, and tumor growth is monitored. The compound's ability to inhibit tumor growth and induce tumor regression is assessed. Pharmacodynamic markers such as mitotic index and apoptosis are measured in tumor tissues. These studies confirm the compound's in vivo efficacy and support its potential as a cancer therapeutic.
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| ADME/Pharmacokinetics |
Kif15-IN-2 has a molecular weight of approximately 411.52 and a molecular formula of C21H25N5O2S. The compound is soluble in DMSO for in vitro assays. For research use, Kif15-IN-2 is typically stored as powder at -20degC for up to 3 years or at 4degC for up to 2 years, and in solvent at -80degC for up to 1 year. Detailed pharmacokinetic parameters such as oral bioavailability, half-life, and tissue distribution have been characterized in preclinical studies for Kif15 inhibitors.
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| Toxicity/Toxicokinetics |
Toxicological data for Kif15-IN-2 are limited. As a research compound, Kif15-IN-2 has not been systematically evaluated for toxicity in preclinical studies. The compound is for research use only and not for human therapeutic use. Standard safety precautions should be followed when handling the compound, including the use of appropriate personal protective equipment. Researchers should consult the Safety Data Sheet (SDS) for specific safety information.
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| References | |
| Additional Infomation |
Kif15-IN-2 (CAS#: 672926-33-9) is a research compound developed as a potent inhibitor of kinesin family member 15 (Kif15) for the study of mitosis and cancer biology. It has a molecular formula of C21H25N5O2S and a molecular weight of approximately 411.52. The compound inhibits Kif15, disrupting spindle assembly and chromosome segregation, leading to mitotic arrest and cell death. Kif15-IN-2 is not approved for clinical use and is available only for research purposes in oncology and cell biology.
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| Molecular Formula |
C₂₀H₂₀N₆O₄S
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|---|---|
| Molecular Weight |
440.4756
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| Exact Mass |
440.126
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| CAS # |
672926-33-9
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| PubChem CID |
60076305
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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 |
1.639
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| LogP |
1.57
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
724
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=C(SC(=N1)NC(=O)[C@H](C(C)C)N2C(=O)C3=CC=CC=C3NC2=O)C4=NN=C(O4)C
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| InChi Key |
OHVKUJISCPKSER-AWEZNQCLSA-N
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| InChi Code |
InChI=1S/C20H20N6O4S/c1-9(2)14(26-18(28)12-7-5-6-8-13(12)22-20(26)29)16(27)23-19-21-10(3)15(31-19)17-25-24-11(4)30-17/h5-9,14H,1-4H3,(H,22,29)(H,21,23,27)/t14-/m0/s1
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| Chemical Name |
(S)-2-(2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)-3-methyl-N-(4-methyl-5-(5-methyl-1,3,4-oxadiazol-2-yl)thiazol-2-yl)butanamide
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| Synonyms |
Kif15-IN-2 Kif15 IN 2 Kif15 IN-2 Kif15-IN 2
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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 : ~20 mg/mL (~45.41 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.54 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 20.0 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 mg/mL (4.54 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 20.0 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 | 2.2703 mL | 11.3513 mL | 22.7025 mL | |
| 5 mM | 0.4541 mL | 2.2703 mL | 4.5405 mL | |
| 10 mM | 0.2270 mL | 1.1351 mL | 2.2703 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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