All AbMole products are for research use only, cannot be used for human consumption.
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.
Curr Cancer Drug Targets. 2023;23(4):293-306.
Combined Inhibition of KIF11 and KIF15 as an Effective Therapeutic Strategy for Gastric Cancer
Ispinesib purchased from AbMole
| 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. |
| Molecular Weight | 517.06 |
| Formula | C30H33ClN4O2 |
| CAS Number | 336113-53-2 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage | 2-8°C, protect from light |
| Related Kinesin Products |
|---|
| AZD4877
AZD4877 is another isostere to Ispinesiband also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. |
| Filanesib TFA
Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. |
| Filanesib hydrochloride
Filanesib (ARRY-520) hydrochloride is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. |
| Eg5-IN-1
Eg5-IN-1 is a potent kinesin family motor protein (Eg5) inhibitor with an IC50 value of 1.97 µM. |
| PVZB-1194
PVZB-1194 is a biphenyl-type inhibitor of kinesin Eg5 that induces apoptosis by inhibiting Eg5 ATPase activity and shows potent kinesin spindle protein (KSP) inhibition only in the presence of microtubules, with anticancer activity. |
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