Ispinesib (SB-715992)

Alias: CK0238273;SB715992; CK-0238273;SB-715992; SB 715992; CK0238273.
Cat No.:V1626 Purity: ≥98%
Ispinesib (formerly also known as CK-0238273, SB-715992), a quinazolinone analog, is anovel,specific and reversible inhibitor of kinesin spindle protein (KSP, a mitotic motor protein) with potential antineoplastic activity.
Ispinesib (SB-715992) Chemical Structure CAS No.: 336113-53-2
Product category: Kinesin
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Ispinesib (formerly also known as CK-0238273, SB-715992), a quinazolinone analog, is a novel, specific and reversible inhibitor of kinesin spindle protein (KSP, a mitotic motor protein) with potential antineoplastic activity. It inhibits KSP with a Ki app of 1.7 nM in a cell-free assay, and exhibits no effects on closely related target proteins such as CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib is derived from quinazolinone with anticancer properties. It acts by selectively inhibiting the mitotic motor protein, kinesin spindle protein (KSP), resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest, and cell death.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Having a Ki app of 1.7 nM, ispinesib is a strong and very selective inhibitor of KSP[1]. BT-474 and MDA-MB-468 cell lines are inhibited by ispinesib (150 nM), with GI50s of 45 and 19 nM, respectively[2]. Ispinesib (SB715992, 15 and 30 nM) causes prostate cancer cells to undergo apoptosis by 1094.88% and 1516.70%, respectively, and suppresses PC-3 prostate cancer cell proliferation by 48.65% and 52.16%. Genes involved in cell cycle arrest and apoptosis are upregulated by ispinenesib, whereas genes involved in cell survival and proliferation are downregulated. Genistein can augment ispinenesib's pro-apoptotic and anti-proliferation properties[3].
ln Vivo
In mice containing tumor xenografts of ER-positive (MCF7), HER2-positive (KPL4, HCC1954, and BT-474), and triple-negative (MDA-MB-468) breast cancer cells, iminetsinib (SCID, 8 mg/kg; nude, 10 mg/kg, q4d × 3) decreases tumor volume by an intraperitoneal injection given three times[2].
Animal Protocol
Dissolved in 10% ethanol, 10% cremophor, and 80% D5W (dextrose 5%); 10 mg/kg for nude mice or 8 mg/kg for SCID mice; i.p. injection on a q4d× schedule, 3 doses, every 4 day
Nude (nu/nu) mice models of MCF7, KPL4, and HCC1954 cells; severe combined immunodeficient (SCID) mice model of MDA-MB-468 cells;
References
[1]. Lad L, et al. Mechanism of inhibition of human KSP by ispinesib. Biochemistry. 2008 Mar 18;47(11):3576-85.
[2]. Purcell JW, et al. Activity of the kinesin spindle protein inhibitor ispinesib (SB-715992) in models of breast cancer. Clin Cancer Res. 2010 Jan 15;16(2):566-76.
[3]. Davis DA, 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 Jan 24;6:22
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C30H33CLN4O2
Molecular Weight
517.06
CAS #
336113-53-2
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
InChi Key
QJZRFPJCWMNVAV-HHHXNRCGSA-N
InChi Code
InChI=1S/C30H33ClN4O2/c1-20(2)27(34(17-7-16-32)29(36)23-12-10-21(3)11-13-23)28-33-26-18-24(31)14-15-25(26)30(37)35(28)19-22-8-5-4-6-9-22/h4-6,8-15,18,20,27H,7,16-17,19,32H2,1-3H3/t27-/m1/s1
Chemical Name
(R)-N-(3-aminopropyl)-N-(1-(3-benzyl-7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-2-methylpropyl)-4-methylbenzamide
Synonyms
CK0238273;SB715992; CK-0238273;SB-715992; SB 715992; CK0238273.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 103 mg/mL (199.2 mM)
Water:<1 mg/mL
Ethanol:103 mg/mL (199.2 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9340 mL 9.6701 mL 19.3401 mL
5 mM 0.3868 mL 1.9340 mL 3.8680 mL
10 mM 0.1934 mL 0.9670 mL 1.9340 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Biological Data
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