KIF2C-IN-1
Based on 1 Customer Validation
KIF2C-IN-1 is a cell-penetrating, selective KIF2C inhibitor with fluorescent properties (Ex/Em = 410/510 nm). KIF2C-IN-1 exhibits notable cytotoxicity and weak inhibitory effects on KIF2A/B. KIF2C-IN-1 prohibits the dissociation of KIF2C from microtubules. KIF2C-IN-1 inhibiting KIF2C reverses cross-resistance to microtubule-targeting agents. KIF2C-IN-1 reduces tumorigenesis in chemoresistant triple-negative breast cancer (TNBC) model in mice with the combination of Paclitaxel (HY-B0015).
For research use only. We do not sell to patients.
- Purity: 98.08%
- Formula: C36H39ClN4O9S
- Molecular Weight:739.23
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Cytoskeleton Compound Library
HY-L060
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Lung Cancer Compound Library
HY-L075
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Pain-Related Compound Library
HY-L139
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Highly Selective Inhibitors Library
HY-L158
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Anti-Drug-Resistant Compound Library
HY-L169
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
All Kinesin Isoforms
More
Biological Activity
KIF2C-IN-1 (compound 7S9) (50 μM) inhibits KIF2C activity by disrupting its dissociation from MTs[1].
KIF2C-IN-1 (0-200 μM, 30 min) increases the molecular interaction between KIF2C and tubulin in a dose-dependent manner, while KIF2C depletion does not alter poly(E) tubulin levels in 4T1 R4 cells[1].
KIF2C-IN-1 (72 h) exhibits notable cytotoxicity against 4T1 S1, R4, and R8 cells (IC50 values of 6.1 μM, 6.8 μM and 4.9 μM respectively)[1].
KIF2C-IN-1 (10 μM, 72 h) restores MT sensitivity to Paclitaxel (400 nM, 72h) in chemoresistant cells (4T1 R4 and 4T1 R8 cells), reducing Paclitaxel IC50 by 11.8- and 8.2-fold, respectively and increasing their sensitivity by 10.5- and 8-fold[1].
KIF2C-IN-1 (1 μM, 14-30 days) induces substantial mitotic defects only with the combined treatment of Paclitaxel (400 nM, 14-30 days) in 4T1 R4 and R8 cells, including prolonged mitotic progression, cytokinesis failure, and mitotic cell death[1].
KIF2C-IN-1 (2 μM) has a synergistic effect with major types of MTAs in chemoresistant cells, which could be a potential strategy to diminish cross-resistance in TNBC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:4T1 S1, R4, and R8 cells
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Concentration:2 μM
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Incubation Time:72 h
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Result:Enhanced the chemosensitivity of R4 and R8 cells to all tested MTAs (Docetaxel (HY-B0011), Ixabepilone (HY-10222), Eribulin (HY-13442), and Vinorelbine (HY-12053)).
Showed the highest synergistic cytotoxic effect with taxane derivatives (Docetaxel and Paclitaxel), increasing sensitivity by more than 90-fold with a CI below 0.5.
Increased chemosensitivity by at least 20-fold in R4 and R8 cells for Ixabepilone, Eribulin and Vinorelbine, with CI values ranging between 0.46 and 0.54.
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Cell Line:4T1 R4 and R8 cells
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Concentration:1 μM, Paclitaxel (400 nM)
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Incubation Time:72 h
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Result:Reduced the IC50 of Paclitaxel in 4T1 R4 and R8 cells by 11.8- and 8.2-fold.
Exhibited increased potency in the presence of a non-lethal dose of Paclitaxel (400 nM), with R4 and R8 cells showing 10.5- and 8-fold increases in sensitivity.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4T1-derived cells (4T1, 4T1 R4, and 4T1 R8 cells, s.c. in the right flank with 5 x 105 cells) induced female BALB/c mice (9-10 weeks old, 18-22 g)[1]
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Dosage:50 mg/kg, Paclitaxel (5 mg/kg for 4T1, 15 mg/kg for 4T1 R4 and R8)
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Administration:Intraperitoneal injection (i.p.), once a day for 5 consecutive days, followed by 2 days of withdrawal
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Result:Inhibited tumor growth by 20.3%, 31.3%, and 62.6% in 4T1-cell-derived tumors in mice treated with Paclitaxel, and the combination, respectively.
Reduced tumor growth at 29%, 41.7%, and 70.2% in mice for R4 cells, treated with KIF2C-IN-1, Paclitaxel, and the combination.
Blocked significant tumor growth by 66.2%, co-treated with Paclitaxel in R8 cells.
Chemical Information
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Appearance Solid
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Molecular Weight 739.23
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Formula C36H39ClN4O9S
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Color Light yellow to yellow
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SMILES
ClC1=CC=C(C2C(C(OC(C)C)=O)=C(C)N=C(S/C3=C\C4=CC=C(OCC(N5CCN(CC)CC5)=O)C=C4)N2C3=O)C=C1.OC(/C=C\C(O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (135.28 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.38 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3528 mL | 6.7638 mL | 13.5276 mL | 33.8190 mL |
| 5 mM | 0.2706 mL | 1.3528 mL | 2.7055 mL | 6.7638 mL | |
| 10 mM | 0.1353 mL | 0.6764 mL | 1.3528 mL | 3.3819 mL | |
| 15 mM | 0.0902 mL | 0.4509 mL | 0.9018 mL | 2.2546 mL | |
| 20 mM | 0.0676 mL | 0.3382 mL | 0.6764 mL | 1.6909 mL | |
| 25 mM | 0.0541 mL | 0.2706 mL | 0.5411 mL | 1.3528 mL | |
| 30 mM | 0.0451 mL | 0.2255 mL | 0.4509 mL | 1.1273 mL | |
| 40 mM | 0.0338 mL | 0.1691 mL | 0.3382 mL | 0.8455 mL | |
| 50 mM | 0.0271 mL | 0.1353 mL | 0.2706 mL | 0.6764 mL | |
| 60 mM | 0.0225 mL | 0.1127 mL | 0.2255 mL | 0.5636 mL | |
| 80 mM | 0.0169 mL | 0.0845 mL | 0.1691 mL | 0.4227 mL | |
| 100 mM | 0.0135 mL | 0.0676 mL | 0.1353 mL | 0.3382 mL |
KIF2C-IN-1 Related Classifications
HY-173522 Related Classifications
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