SB-715992 (Ispinesib)

Cas No.:	336113-53-2
Chemical Name:	Benzamide,N-(3-aminopropyl)-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl]-2-methylpropyl]-4-methyl-
Synonyms:	Benzamide,N-(3-aminopropyl)-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl]-2-methylpropyl]-4-methyl-;Ispinesib (SB-715992);Ispinesib;Ispinesib (SB-715992,CK-0238273);N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxoquinazolin-2-yl)-2-methylpropyl]-4-methylbenzamide;N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl]-2-met...;SB-715992;Ispinesib mesilate;Ispinesib mesylate;SB 715992;UNII-BKT5F9C2NI;N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylmethyl)-2-quinazolinyl]-2-methylpropyl]-4-methylbenzamide
SMILES:	O=C1N(CC2=CC=CC=C2)C([C@@H](C(C)C)N(CCCN)C(C3=CC=C(C)C=C3)=O)=NC4=CC(Cl)=CC=C14
Formula:	C30H33N4O2Cl
M.Wt:	517.06162
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Ispinesib is a specific inhibitor of KSP, with a Ki app of 1.7 nM.
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].
In Vitro:	Ispinesib is a potent, highly specific inhibitor of KSP, with a Ki app of 1.7 nM[1]. Ispinesib (150 nM) inhibits BT-474 and MDA-MB-468 cell lines, with GI50s of 45 and 19 nM, respectively[2]. Ispinesib (SB715992, 15 and 30 nM) suppresses the proliferation of PC-3 prostate cancer cell by 48.65% and 52.16%, and induces apoptosis of prostate cancer cell by 1094.88% and 1516.70%, respectively. Ispinesib up regulates genes responsible for apoptosis and cell cycle arrest, and down regulates genes responsible for cell proliferation and survival. The anti-proliferation and pro-apoptotic activities of Ispinesib can be enhanced by genistein[3].