Art. -Nr.: HY-50759

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Ispinesib

(Synonyms: SB-715992; CK-0238273)

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

Ispinesib is a specific inhibitor of kinesin spindle protein (KSP), with a K_{i app} of 1.7 nM.

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Reinheit: 99.62%
CAS. Nr.: 336113-53-2
Formel: C₃₀H₃₃ClN₄O₂
Molecular Weight:517.06

Speicherung:

4°C, protect from light

* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Ispinesib Chemical Structure

CAS. Nr.: 336113-53-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Ispinesib is a specific inhibitor of kinesin spindle protein (KSP), with a K_{i app} of 1.7 nM.

IC₅₀ & Target^[1]

KSP

1.7 nM (Ki app)

LC3

Alle Kinesin Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	GI₅₀	80 nM Compound: 1	Growth inhibition of human BxPC3 cells after 72 hrs by Alamar blue assay Growth inhibition of human BxPC3 cells after 72 hrs by Alamar blue assay	[PMID: 23394180]
BXPC-3	GI₅₀	80 nM Compound: 54	Antiproliferative activity against human BxPC3 cells after 72 hrs by Alamar blue assay Antiproliferative activity against human BxPC3 cells after 72 hrs by Alamar blue assay	[PMID: 22248262]
HCT-116	GI₅₀	25 nM Compound: 1	Growth inhibition of human HCT116 cells after 72 hrs by Alamar blue assay Growth inhibition of human HCT116 cells after 72 hrs by Alamar blue assay	[PMID: 23394180]
HCT-116	GI₅₀	25 nM Compound: 54	Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay	[PMID: 22248262]
HCT-116	IC₅₀	1.1 nM Compound: 1	Growth inhibition of human HCT116 cells after 72 hrs by MTS assay Growth inhibition of human HCT116 cells after 72 hrs by MTS assay	[PMID: 26396688]
HeLa	IC₅₀	1 μM Compound: SB715992	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 24184776]
K562	GI₅₀	71 nM Compound: 54	Antiproliferative activity against human K562 cells after 72 hrs by Alamar blue assay Antiproliferative activity against human K562 cells after 72 hrs by Alamar blue assay	[PMID: 22248262]
LNCaP	GI₅₀	22 nM Compound: 1	Growth inhibition of human LNCAP cells after 72 hrs by Alamar blue assay Growth inhibition of human LNCAP cells after 72 hrs by Alamar blue assay	[PMID: 23394180]
MCF7	IC₅₀	1.3 μM Compound: SB715992	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 24184776]
NCI-H1299	GI₅₀	82 nM Compound: 1	Growth inhibition of human NCI-H1299 cells after 72 hrs by Alamar blue assay Growth inhibition of human NCI-H1299 cells after 72 hrs by Alamar blue assay	[PMID: 23394180]
NCI-H1299	GI₅₀	82 nM Compound: 54	Antiproliferative activity against human NCI-H1299 cells after 72 hrs by Alamar blue assay Antiproliferative activity against human NCI-H1299 cells after 72 hrs by Alamar blue assay	[PMID: 22248262]
PC-3	GI₅₀	50 nM Compound: 1	Growth inhibition of human PC3 cells after 72 hrs by Alamar blue assay Growth inhibition of human PC3 cells after 72 hrs by Alamar blue assay	[PMID: 23394180]

In Vitro

Ispinesib is a potent, highly specific inhibitor of KSP, with a K_{i app} of 1.7 nM^[1].
Ispinesib (150 nM) inhibits BT-474 and MDA-MB-468 cell lines, with GI₅₀s of 45 and 19 nM, respectively^[2].
Ispinesib (SB715992, 15 and 30 nM) suppresses the proliferation of PC-3 prostate cancer cell by 48.65% and 52.16%, and induces apoptosis of prostate cancer cell by 1094.88% and 1516.70%, respectively. Ispinesib up regulates genes responsible for apoptosis and cell cycle arrest, and down regulates genes responsible for cell proliferation and survival. The anti-proliferation and pro-apoptotic activities of Ispinesib can be enhanced by genistein^[3].

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

In Vivo

Ispinesib (SCID, 8 mg/kg; nude, 10 mg/kg, q4d × 3) reduces tumor volume in mice bearing tumor xenografts of ER-positive (MCF7), HER2-positive (KPL4, HCC1954, and BT-474), and triple-negative (MDA-MB-468) breast cancer cells via i.p. one dose every 4 days repeated three times^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 336113-53-2
Appearance Solid
Molecular Weight 517.06
Formel C₃₀H₃₃ClN₄O₂
Color White to light yellow
SMILES

O=C1N(CC2=CC=CC=C2)C([C@@H](C(C)C)N(CCCN)C(C3=CC=C(C)C=C3)=O)=NC4=CC(Cl)=CC=C14
Synonyms

SB-715992; CK-0238273
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Publications (7)

All Flow CytometryCell Proliferation/Viability AssayIn Vivo Efficacy Study

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Journal Impact Factor

Redox Biol

Intracellular ion and protein nanoparticle-induced osmotic pressure modify astrocyte swelling and brain edema in response to glutamate stimuli. [Abstract]

2019 Feb:21:101112. PMID: 30685709
Cancer Lett

KIF11 inhibitors filanesib and ispinesib inhibit meningioma growth in vitro and in vivo. [Abstract]

2021 May 28:506:1-10. PMID: 33652084

Ispinesib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2021 May 28:506:1-10. [Abstract]

Ispinesib impaired cell cycle progression.Cell cycle distribution of MGM cells treated with 10 nM Filanesib (10 nM) or Ispinesib (10 nM) after 24, 48, and 72 h.

Ispinesib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2021 May 28:506:1-10. [Abstract]

Ispinesib (10 nM; 72 h) induced cell apoptosis. Filanesib or ispinesib treatment induced cell death by the accumulation of cells in early and late-stage apoptosis in all MGM cell lines measured by Annexin V (FITC)/PI staining (left). Numbers indicate the percentage of Annexin V-positive cells (right).

Ispinesib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2021 May 28:506:1-10. [Abstract]

NCH93 tumor-bearing mice were randomized into three groups after reaching a tumor size of 200 mm³. Treatment with vehicle (DMSO), filanesib (10 mg/kg body weight), or Ispinesib (5 mg/kg; i.p.) was initiated on day 0. Mice were treated once every three days on five occasions. KIF11i significantly inhibited NCH93 tumor growth in SCID mice.
Cancers (Basel)

Targeting the EGFR and Spindle Assembly Checkpoint Pathways in Oral Cancer: A Plausible Alliance to Enhance Cell Death. [Abstract]

2024 Nov 5;16(22):3732. PMID: 39594688

Ispinesib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2024 Nov 5;16(22):3732. [Abstract]

Ispinesib (1.875-30 nM) + Cetuximab (15-240 nM) combinations potentiate cytotoxicity in SCC-25 cell lines. Cell viability (%) after 48 h of exposure to single or combination therapies was determined by MTT assay based on three independent experiments.

Ispinesib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2024 Nov 5;16(22):3732. [Abstract]

Ispinesib (1.875 nM; 24 h) + Cetuximab (240 nM; 24 h) promoted increased cell death in SCC-25 oral cancer cells.
Gene

Targeting Eg5 using Arry520 combats gastric cancer by inducing monopolar spindles. [Abstract]

2025 Apr 3:955:149458. PMID: 40187619
Urol Oncol

Identification of the KIF and MCM protein families as novel targets for combination therapy with CDK4/6 inhibitors in bladder cancer. [Abstract]

2023 May;41(5):253.e11-253.e20. PMID: 36813612
Preprints

2023 Sep 30.
bioRxiv

Multiplexed single-cell lineage tracing of mitotic kinesin inhibitor resistance in glioblastoma. [Abstract]

2023 Sep 12:2023.09.09.557001. PMID: 37745469

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 116.67 mg/mL (225.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.9340 mL

9.6701 mL

19.3401 mL

5 mM

0.3868 mL

1.9340 mL

3.8680 mL

10 mM

0.1934 mL

0.9670 mL

1.9340 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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, 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

Protokoll

Kinase Assay^[1]

Kinesin specificity analysis is carried out using a pyruvate kinase−lactate dehydrogenase detection system that couples the production of ADP to oxidation of NADH. Absorbance changes are monitored at 340 nm. Steady-state studies using nanomolar concentrations of KSP are performed using a sensitive fluorescence-based assay utilizing a pyruvate kinase, pyruvate oxidase, and horseradish peroxidase coupled detection system that couples the generation of ADP to oxidation of Amplex Red to fluorescent resorufin. Generation of resorufin is monitored by fluorescence (λexcitation = 520 nm and λemission= 580 nm). Steady-state biochemical experiments are performed in PEM25 buffer [25 mM Pipes-K⁺ (pH 6.8), 2 mM MgCl₂, 1 mM EGTA] supplemented with 10 µM paclitaxel for experiments involving microtubules. The IC₅₀ for steady-state inhibition is determined at 500 µM ATP, 5 µM MTs, and 1 nM KSP in PEM25 buffer. K_{i app} (apparent inhibitor dissociation constant) estimates of Ispinesib are extracted from the concentration-response curves, with explicit correction for enzyme concentration^[1].

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

Cell Assay^[3]

PC-3 prostate cancer cells are seeded in 96 well plates at a density of 4 × 10³ cells/well. PC-3 cells are incubated for 24 hours to allow attachment to the surface of each well of the tissue culture plate. Then, the cells are treated with varying concentration of reagents and incubated for 1 to 3 days. First, PC-3 cells are treated with 15 and 30 nM of Ispinesib, respectively. Second, PC-3 cells are subjected to combinational treatments with 7.5 or 10 nM of Ispinesib plus 30 μM of genistein. Finally, PC-3 cells are pre-treated with 30 μM of genistein for 24 hours followed by treatment with 15 nM of Ispinesib. Control cells are treated with 0.3 mM Na₂CO₃ (vehicle control). After treatment, PC3 cells are incubated at 37°C with MTT (0.5 mg/mL) for 2 hours and isopropyl alcohol at room temperature for 1 hour. The spectrophotometric absorbance of each sample is then determined by using ULTRA Multifunctional Micro Plate Reader at 595 nm^[3].

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

Animal Administration^[2]

Mice with a tumor volume of ∼250 mm³ receive a single dose of Ispinesib (10 mg/kg). Tumors are dissected, fixed in 10% buffered formalin, and embedded in paraffin, and 5-μm tissue sections are prepared. Antigen retrieval is done by boiling in 50 mM citrate buffer (pH 5.5), and sections are then incubated in 3% hydrogen peroxide, washed in PBS-0.1% Tween, and blocked in 10% goat serum. Phospho-histone H3 (PH3) antibody is detected using Alexa Fluor 488 secondary antibody. Images are taken with a microscope at ×10 magnification and captured using MetaMorph software to quantify PH3 expression by computing the area ratio of PH3-positive cells per total cells. Ki67/cleaved caspase-3 staining is done. Nonfluorescent images are taken on an Olympus BX41 microscope at ×20 magnification^[2].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 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]. Lad L, et al. Mechanism of inhibition of human KSP by ispinesib. Biochemistry. 2008 Mar 18;47(11):3576-85. [Content Brief]

[2]. Purcell JW, et al. Activity of the kinesin spindle protein inhibitor ispinesib (SB-715992) in models of breast cancer. Clin Cancer Res. 2010 Jan 15;16(2):566-76. [Content Brief]

[3]. Davis DA, et al. Increased therapeutic potential of an experimental anti-mitotic inhibitor SB715992 by genistein in PC-3 human prostate cancer cell line. BMC Cancer. 2006 Jan 24;6:22. [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	1.9340 mL	9.6701 mL	19.3401 mL	48.3503 mL
	5 mM	0.3868 mL	1.9340 mL	3.8680 mL	9.6701 mL
	10 mM	0.1934 mL	0.9670 mL	1.9340 mL	4.8350 mL
	15 mM	0.1289 mL	0.6447 mL	1.2893 mL	3.2234 mL
	20 mM	0.0967 mL	0.4835 mL	0.9670 mL	2.4175 mL
	25 mM	0.0774 mL	0.3868 mL	0.7736 mL	1.9340 mL
	30 mM	0.0645 mL	0.3223 mL	0.6447 mL	1.6117 mL
	40 mM	0.0484 mL	0.2418 mL	0.4835 mL	1.2088 mL
	50 mM	0.0387 mL	0.1934 mL	0.3868 mL	0.9670 mL
	60 mM	0.0322 mL	0.1612 mL	0.3223 mL	0.8058 mL
	80 mM	0.0242 mL	0.1209 mL	0.2418 mL	0.6044 mL
	100 mM	0.0193 mL	0.0967 mL	0.1934 mL	0.4835 mL

Keywords

Ispinesib

7 Cited Publications

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Ispinesib

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Ispinesib

Alle Kinesin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ispinesib

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Ispinesib

Alle Kinesin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ispinesib Related Classifications

Art. -Nr.: HY-50759