Art. -Nr.: HY-173522

KIF2C-IN-1

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KIF2C-IN-1 is a cell-penetrating, selective KIF2C inhibitor with fluorescent properties (E_x/E_m = 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).

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Reinheit: 98.08%
Formel: C₃₆H₃₉ClN₄O₉S
Molecular Weight:739.23

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

KIF2C-IN-1 Chemical Structure

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Kinesin Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:

4T1 S1, R4, and R8 cells
Concentration:

2 μM
Incubation Time:

72 h
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.

Cell Viability Assay^[1]

Cell Line:

4T1 R4 and R8 cells
Concentration:

1 μM, Paclitaxel (400 nM)
Incubation Time:

72 h
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.

In Vivo

KIF2C-IN-1 (compound 7S9) (50 mg/kg, i.p., once daily, five days per week, for two consecutive weeks) synergistically enhances the anti-tumor effects of Paclitaxel in both chemosensitive (4T1 S1) and chemoresistant (4T1 R4 and R8 ) cells of BALB/c mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage:

50 mg/kg, Paclitaxel (5 mg/kg for 4T1, 15 mg/kg for 4T1 R4 and R8)
Administration:

Intraperitoneal injection (i.p.), once a day for 5 consecutive days, followed by 2 days of withdrawal
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

Appearance Solid
Molecular Weight 739.23
Formel C₃₆H₃₉ClN₄O₉S
Color Light yellow to yellow
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pao YS, et al. KIF2C promotes paclitaxel resistance by depolymerizing polyglutamylated microtubules. Dev Cell. 2025 Mar 25:S1534-5807(25)00151-0. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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KIF2C-IN-1

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Anti-Drug-Resistant Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Kinesin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

KIF2C-IN-1

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Anti-Drug-Resistant Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Kinesin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

KIF2C-IN-1 Related Classifications

HY-173522 Related Classifications