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Ispinesib

Ispinesib Structure
Ispinesib
  • CAS No.336113-53-2
  • Chemical Name:Ispinesib
  • CBNumber:CB01565568
  • Molecular Formula:C30H33ClN4O2
  • Formula Weight:517.06
  • MOL File:336113-53-2.mol
Ispinesib Property
  • 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
  • optical activity [α]/D +315 to +375°, c =0.5 in chloroform-d
  • NCI Dictionary of Cancer Terms ispinesib; SB-715992
  • FDA UNII BKT5F9C2NI
  • NCI Drug Dictionary ispinesib
  • UNSPSC Code 12352200
  • NACRES NA.77
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H227
  • Precautionary statements P501-P210-P280-P370+P378-P403+P235

Ispinesib Chemical Properties,Usage,Production

  • Uses 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]
  • 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].
  • 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].

  • IC 50 KSP: 1.7 nM (Ki app)
  • 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.
Ispinesib Preparation Products And Raw materials
Raw materials
Preparation Products
Ispinesib Suppliers
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Ispinesib Spectrum
336113-53-2, IspinesibRelated Search:
  • Apis
  • Pharmaceuticals
  • Intermediates & Fine Chemicals
  • Inhibitors
  • Chiral Reagents
  • 抑制剂
  • 生物试剂
  • 药靶配体
  • 细胞生物学试剂
  • 小分子抑制剂，天然产物
  • 细胞骨架信号
  • 小分子抑制剂
  • C30H33ClN4O2
  • 伊斯平斯,10 MM DMSO 溶液
  • (R)-N-(3-氨基丙基)-N-[1-(3-苄基-7-氯-4-氧代-3,4-二氢-2-喹唑啉)-2-甲基丙基]-4-甲基苯甲酰胺
  • (R)-N-(3-氨基丙基)-N-(1-(3-苄基-7-氯-4-氧代-3,4-二氢喹唑啉-2-基)-2-甲基丙基)-4-甲基苯甲酰胺
  • 7-二氢-1-甲基-7-氧代-3-丙基-1H-吡唑并[4
  • 3-D]嘧啶-5-基)-N-[2-(1-甲基-2-吡咯烷基)乙基]-4-丙氧基苯磺酰胺
  • KSP(HSEG5)特异性抑制剂(ISPINESIB)
  • (抗癌类)伊斯平斯
  • 伊斯平斯
  • 伊匹尼塞
  • 336113-53-2
  • Ispinesib, 10 mM in DMSO
  • (R)-N-(3-Aminopropyl)-N-[1-(3-benzyl-7-chloro-4-oxo-3,4-dihydro-2-quinazolinyl)-2-methylpropyl]-4-methylbenzamide
  • ISPINESIB;SB-715992;SB715992
  • CS-376
  • 3-(6
  • (R)-N-(3-Aminopropyl)-N-(1-(3-benzyl-7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-2-methylpropyl
  • Ispinesib, >=98%
  • SB715992 (Ispinesib)
  • N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl]-2-methylpropyl]-4-methylbenzamide Ispinesib(SB-715992)
  • Ispinesib N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl]-2-methylpropyl]-4-methylbenzamide
  • CK0238273
  • (R)-N-(3-aminopropyl)-N-(1-(3-benzyl-7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-2-methylpropyl)-4-methylbenzamide
  • BenzaMide, N-(3-aMinopropyl)-N-((1R)-1-(7-chloro-3,4-dihydro-4-oxo-3-(phenylMethyl)-2-quinazolinyl)-2-Methylprop
  • Ispinesib (SB-715992)
  • Ispinesib Mesilate(SB-715992)
  • Ispinesib (SB-715992 /CK0238273)
  • SB-71599
  • Ispinesib2
  • Unii-bkt5F9C2ni
  • Benzamide, N-(3-aminopropyl)-N-((1R)-1-(7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl)-2-methylpropyl)-4-methyl-
  • SB 715992
  • N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl]-2-methylpropyl]-4-methylbenzamide
  • Ispinesib

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