| Size | Price | Stock | Qty |
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| 10mg |
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| ln Vitro |
KIF2C-IN-1 (compound 7S9) (50 μM) inhibits the activity of KIF2C by interfering with the dissociation of KIF2C from microtubules [1]. KIF2C-IN-1 (0–200 μM, 30 min) enhances the molecular interaction between KIF2C and tubulin in a dose-dependent manner, while the loss of KIF2C does not alter the level of poly(E) tubulin in 4T1 R4 cells [1]. KIF2C-IN-1 (72 h) showed significant cytotoxicity to 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) restored the sensitivity of drug-resistant cells (4T1 R4 and 4T1 R8 cells) to paclitaxel (400 nM, 72 h), reducing the paclitaxel IC50 by 11.8-fold and 8.2-fold, respectively, and increasing their sensitivity by 10.5-fold and 8-fold, respectively [1]. KIF2C-IN-1 (1 μM, 14–30 days) only induced significant mitotic defects in 4T1 R4 and R8 cells, including prolonged mitotic progression, cytokinesis failure, and mitotic cell death, when used in combination with paclitaxel (400 nM, 14–30 days) [1]. KIF2C-IN-1 (2 μM) synergistically interacts with the major MTA types in chemotherapeutic-resistant cells, which may be a potential strategy to reduce TNBC cross-resistance [1].
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| ln Vivo |
KIF2C-IN-1 (compound 7S9) (50 mg/kg, intraperitoneal injection, once daily, five days a week for two consecutive weeks) can synergistically enhance the antitumor effect of paclitaxel on chemotherapeutic cells (4T1 S1) and chemotherapeutic resistant cells (4T1 R4 and R8) in BALB/c mice [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: 4T1 S1, R4 and R8 cells Tested Concentrations: 2 μM Incubation Duration: 72 hours Experimental Results: Enhanced the chemosensitivity of R4 and R8 cells to all tested MTAs (docetaxel, ixapril, eribulin and vinorelbine). Showed the highest synergistic cytotoxicity with taxane derivatives (docetaxel and paclitaxel), increasing sensitivity by more than 90-fold with CI values below 0.5. Ixapril, eribulin and vinorelbine increased the chemosensitivity of R4 and R8 cells by at least 20-fold with CI values between 0.46 and 0.54. Cell viability assay [1] Cell Types: 4T1 R4 and R8 cells Tested Concentrations: 1 μM paclitaxel (400 nM) Incubation Duration: 72 hours Experimental Results: The IC50 values of paclitaxel in 4T1 R4 and R8 cells decreased by 11.8-fold and 8.2-fold, respectively. In the presence of a non-lethal dose of paclitaxel (400 nM), its potency was enhanced, and the sensitivity of R4 and R8 cells increased by 10.5-fold and 8-fold, respectively. |
| Animal Protocol |
Animal/Disease Models:Female BALB/c mice (9-10 weeks old, 18-22 g) were induced with 4T1-derived cells (4T1, 4T1 R4 and 4T1 R8 cells, injected subcutaneously into the right abdomen at a dose of 5 x 10⁵ cells) [1]
Doses: 50 mg/kg, paclitaxel (5 mg/kg for 4T1 cells, 15 mg/kg for 4T1 R4 and R8 cells) Route of Administration: Intraperitoneal injection (ip), once daily for 5 days, followed by a 2-day break Experimental Experimental Results: In mice treated with paclitaxel, the growth of 4T1 cell-derived tumors was inhibited by 20.3%, 31.3% and 62.6%, respectively. Combined administration reduced the growth of R4 cell tumors in mice by 29%, 41.7% and 70.2%, respectively. In R8 cells, combination therapy with paclitaxel significantly inhibited tumor growth by 66.2%. |
| References |
| Molecular Formula |
C36H39CLN4O9S
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|---|---|
| Molecular Weight |
739.23
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| Appearance |
Light yellow to yellow solid
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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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| 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 Note: 请将本产品存放在密封保护的环境中，避免受潮。 |
| 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 (~135.28 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (3.38 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Suspended solution; Need ultrasonic.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3528 mL | 6.7638 mL | 13.5276 mL | |
| 5 mM | 0.2706 mL | 1.3528 mL | 2.7055 mL | |
| 10 mM | 0.1353 mL | 0.6764 mL | 1.3528 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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