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Ispinesib (SB-715992) - 10mM in DMSO, high purity , CAS No.336113-53-2(DMSO), Kinesin-like protein 1 inhibitor

COA

Grade & Purity:

10mM in DMSO

Cas Number: 336113-53-2(DMSO)
Molecular Weight: 517.06

In stock

Item Number

I408840

Grouped product items
SKU	Size	Availability	Price	Qty
I408840-1ml	1ml	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$352.90

Kinesin Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms	CK0238273 \| (R)-N-(3-aminopropyl)-N-(1-(3-benzyl-7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-2-methylpropyl)-4-methylbenzamide
Specifications & Purity	10mM in DMSO
Biochemical and Physiological Mechanisms	Ispinesib (SB-715992, CK0238273) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with K_{i app} of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib induces mitotic ar
Storage Temp	Store at -80°C
Shipped In	Dry ice packs + Cold packs This product requires cold chain shipping. Ground and other economy services are not available.
Action Type	INHIBITOR
Mechanism of action	Kinesin-like protein 1 inhibitor
Product Description	Information Ispinesib (SB-715992) Ispinesib (SB-715992, CK0238273) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with K i app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib indu In vitro Ispinesib is a potent, allosteric, reversible, and specific inhibitor of KSP, which changes the binding property of KSP to microtubules and disturbs its movement by inhibiting ADP release without altering the release of the KSP-ADP complex from the microtubule. Ispinesib shows potent cytotoxic activity in a panel of tumor cell lines, including Colo205, Colo201, HT-29, M5076, Madison-109, and MX-1, with IC50 of 1.2 nM to 9.5 nM. In PC-3 prostate cancer cells, Ispinesib (15 nM and 30 nM) blocks cell proliferation and induces apoptosis by regulating the expression levels of genes that controls apoptosis, cell proliferation, cell cycle, and cell signaling, such as EGFR, p27, p15, and IL-11. In a panel of 53 breast cell lines, Ispinesib (7.4 nM–600 nM) demonstrates broad inhibitory activity. In BT-474 and MDA-MB-468 cells, Ispinesib (150 nM) induces apoptosis, as revealed by a higher proportion of apoptotic cells, lower antiapoptotic Bcl-X_L level, and higher proapoptotic Bax and Bid levels. In vivo Ispinesib (4.5 mg/kg–15 mg/kg) exhibits inhibitory effects against Colo205, Colo201, HT-29, but not MX-1 cells, in mouse xenograft models. SB-715992 (6 mg/kg–10 mg/kg ) also inhibits murine solid tumors, including Madison 109 lung carcinoma, M5076 sarcoma, as well as L1210 and P388 leukemias. In mice xenograft models of breast cancer cells MCF-7, HCC1954, MDA-MB-468, and KPL4, Ispinesib (8 mg/kg–10 mg/kg) inhibits tumor growth. Cell Data cell lines：MiaPaCa-2, PANC-1, and GIST882 cells Concentrations：0.085 nM–33 µM Incubation Time：72 hours Powder Purity:≥95%

Product Properties

ALogP	5.259
hba_count	3
HBD Count	1
Rotatable Bond	9

Associated Targets(Human)

KIF11 Tchem Kinesin-like protein KIF11 (5 Activities)

Discover Target: KIF11

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (1 Activities)

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Smiles	CC(C)C(N(CCCN)C(=O)C1=CC=C(C)C=C1)C2=NC3=C(C=CC(=C3)Cl)C(=O)N2CC4=CC=CC=C4
Molecular Weight	517.06
Reaxy-Rn	21642425
Reaxys-RN_link_address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21642425&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

DMSO(mg / mL) Max Solubility	103
DMSO(mM) Max Solubility	199.2
Water(mg / mL) Max Solubility	<1

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