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Ispinesib

Ispinesib structure

CAS No:
336113-53-2
Formula:
C30H33ClN4O2
Chemical Name:
Ispinesib
Synonyms:
Ispinesib;N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl]-2-methylpropyl]-4-methylbenzamide;SB 715992;Benzamide, N-(3-aminopropyl)-N-((1R)-1-(7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl)-2-methylpropyl)-4-methyl-;Unii-bkt5F9C2ni;Ispinesib2;SB-71599;Ispinesib (SB-715992 /CK0238273)
Categories:
Biochemical Engineering > Inhibitors

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Description

Ispinesib is a specific inhibitor of KSP, with a Ki app of 1.7 nM.

Ispinesib Basic Attributes

Molecular Weight：

517.08

Exact Mass：

516.229187

Characteristics

PSA：

XLogP3：

5.3

Density：

1.2±0.1 g/cm3

Boiling Point：

707.986°C at 760 mmHg

Flash Point：

382.0±35.7 °C

Refractive Index：

1.619

Ispinesib Use and Manufacturing

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]

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Ispinesib

CAS No.: 336113-53-2

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