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HomeProduct name listIspinesib

Ispinesib

Ispinesib Structural

What is Ispinesib?

The Uses of Ispinesib

Ispinesib is the first potent, highly specific small-molecule inhibitor of KSP tested for the treatment of human disease. Anticancer agent.

The Uses of Ispinesib

The kinesin-like spindle protein Eg5 (also known as kinesin-5, kinesin family protein 11, or Kif11) is a motor protein that is essential for establishing a bipolar spindle during mitosis both in normal and tumor cells. Ispinesib is a cell-permeable, allosteric inhibitor of Eg5 (Ki app = 2.3 nM) with >10,000-fold selectivity for Eg5 over a range of other mitotic kinesins. It induces a monopolar spindle phenotype, leading to the activation of a spindle assembly checkpoint, mitotic arrest, and subsequent cell death (GI50s = 22-82 nM in colon, pancreas, prostrate, and lung cancer cells in vitro). At 10 mg/kg, ispinesib produces tumor regression of breast cancer cell xenografts in mice. It has also been used to halt the growth of treatment-resistant glioblastoma tumor-initiating cells, to prevent tumor initiation and self-renewal of a cancer stem cell population (EC50 = 1.15 nM), and to reduce glioma cell invasion.[Cayman Chemical]

What are the applications of Application

Ispinesib is an allosteric, specific reversible inhibitor of Eg5

Definition

ChEBI: N-(3-aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-2-quinazolinyl]-2-methylpropyl]-4-methylbenzamide is a member of benzamides.

Biological Activity

ispinesib (sb-715992) is a selective inhibitor of ksp with ic50 value of 0.5 nm [1].kinesin spindle protein (ksp) is a kinesin motor protein and plays an important role in the formation of a bipolar mitotic spindle and cell cycle progression through mitosis. it has been shown that abnormal expression of ksp is correlated with a variety of human cancers and its inhibitors may be a promising anticancer agent [2] [3].ispinesib (sb-715992) is a potent ksp inhibitor and often combines with chemotherapy drugs to tumor treatment. when tested with a panel of 23 tumor cell lines, ispinesib (sb-715992) treatment showed high activity to inhibit ksp in most of the cell lines while only rh18 having an ic50 value greater than 1 μm (median ic50=4.1 nm, maximum ic50=0.5 nm) by using pptp method [1]. in a panel of 53 breast cell lines, ispinesib (sb-715992) exhibits broad antiproliferative activity and up-regulated the expression of both mitotic and apoptotic markers in mda-mb-468 cell line [2]. when tested with pc-3 cells, ispinesib (sb-715992) treatment inhibits cell proliferation, inducs cell apoptosis and up-regulated the expressions of genes that related to the control of cell proliferation, cell cycle, cell signaling pathways and apoptosis [3].in mouse model with 26 tumor cells subcutaneous xenograft, administration of ispinesib (sb-715992) inducs markedly tumor growth delay with the percent of 88% (23/26) and maintained completed response (cr) in the rhaboid tumor, wilms tumor and ewing sarcoma xenograft mouse model [1].

storage

Store at -20°C

References

[1]. carol, h., et al., initial testing (stage 1) of the kinesin spindle protein inhibitor ispinesib by the pediatric preclinical testing program. pediatr blood cancer, 2009. 53(7): p. 1255-63.
[2]. purcell, j.w., et al., activity of the kinesin spindle protein inhibitor ispinesib (sb-715992) in models of breast cancer. clin cancer res, 2010. 16(2): p. 566-76.
[3]. davis, d.a., 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. 6: p. 22.

Properties of Ispinesib

Melting point: 89 - 92°C
Boiling point: 708.0±70.0 °C(Predicted)
Density  1.21±0.1 g/cm3(Predicted)
storage temp.  -20°C Freezer, Under inert atmosphere
solubility  Chloroform (Slightly), Methanol (Slightly)
form  Solid
pka 9.65±0.10(Predicted)
color  White to Off-White

Safety information for Ispinesib

Signal word Warning
Pictogram(s)
ghs
Flame
Flammables
GHS02
ghs
Corrosion
Corrosives
GHS05
ghs
Skull and Crossbones
Acute Toxicity
GHS06
ghs
Health Hazard
GHS08
GHS Hazard Statements H227:Flammable liquids
Precautionary Statement Codes P210:Keep away from heat/sparks/open flames/hot surfaces. — No smoking.
P280:Wear protective gloves/protective clothing/eye protection/face protection.
P370+P378:In case of fire: Use … for extinction.
P403+P235:Store in a well-ventilated place. Keep cool.

Computed Descriptors for Ispinesib

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