Free shipping on all orders over $ 500

Ispinesib

Cat. No. M1786
Ispinesib Structure
Synonym:

SB-715992, CK0238273

Size Price Availability Quantity
10mg USD 250 In stock
50mg USD 790 In stock
Bulk Inquiry?

Quality Control
Biological Activity

Ispinesib (SB-715992), a potent and selective small molecule inhibitor of KSP, functions by inhibiting KSP ATPase and is 40000 times more selective for KSP compared to other kinesins. In preclinical studies, ispinesib inhibited growth in a wide range of human and murine cell lines with IC50 values of 1.2-9.5nm. Treatment of SKOV3 ovarian tumour cells in vitro with 20nm of ispinesib, or a Colo 205 colon cancer murine xenograft model with 30mgkg-1 of intraperitoneal ispinesib, caused mitotic arrest with cells demonstrating unseparated centrosomes and monopolar mitotic spindles. Tumour growth delay was observed in xenograft models of colon (HT29, Colo201, Colo205), non-small cell lung (Calu-3) and pancreatic (Panc-01) cancers.

Protocol
Cell Experiment
Cell lines BT-474 and MDA-MB-468 cells line
Preparation method Cell lines were obtained from the American Type Culture Collection and from collections developed by Drs. Steve Ethier and Adi Gazdar. KPL4 was kindly provided by Dr J. Kurebayashi (Kawasaki Medical School, Kurashiki, Okayama, Japan). Cell culture reagents were from Cellgro-Mediatech. Cells were plated in log phase of growth in 96-well plates and treated for 72 h with ispinesib at concentrations of 3.3 × 10−5 to 8.5 × 10−11 mol/L. Cell growth was measured using CellTiter-Glo (Promega), and luminescence was recorded using BioTek FLx800. Data were analyzed according to the method described previously by the National Cancer Institute/NIH Developmental Therapeutics Program Human Tumor Cell Line Screen Process. The GI50 value is the drug concentration that results in 50% growth inhibition after 72 h of drug exposure relative to control.
Concentrations 0~1000 n M
Incubation time 72 h
Animal Experiment
Animal models MCF-7, BT-474 and MDA-MB-468 xenograft model in nude mice or SCID mice
Formulation formulated in 10% ethanol, 10% cremophor, and 80% D5W (dextrose 5%)
Dosages q4d×3 schedule at 10 mg/kg in nu/nu mice or 8 mg/kg in SCID mice
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 517.06
Formula C30H33ClN4O2
CAS Number 336113-53-2
Purity >99%
Solubility DMSO
Storage at -20°C
References

Activity of the kinesin spindle protein inhibitor ispinesib (SB-715992) in models of breast cancer.
Purcell et al. Clin Cancer Res. 2010 Jan 15;16(2):566-76. PMID: 20068098.

Thermodynamics of nucleotide and inhibitor binding to wild-type and ispinesib-resistant forms of human kinesin spindle protein.
Sheth et al. Biochemistry. 2009 Nov 24;48(46):11045-55. PMID: 19824700.

Related Kinesin Products
Monastrol

Monastrol is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles.

AZD4877

AZD4877 is a synthetic kinesin spindle protein (KSP) inhibitor with potential antineoplastic activity.

ARRY-520

ARRY-520 is a potent and selective kinesin spindle protein (KSP) inhibitor with an IC50 of 15 nM for A2780, CP70 and 01-28 cell lines in vitro.

MPI-0479605

MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases.

GSK923295

GSK923295 is an allosteric inhibitor of CENP-E with Ki value of 3.2 nM.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ispinesib, SB-715992, CK0238273 supplier, Kinesin, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.