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Filanesib

Catalog No. TQ0318 CAS 885060-09-3

Synonyms: ARRY-520, ARRY 520

Filanesib (ARRY 520) is a selective inhibitor of kinesin spindle protein (KSP, IC50 = 6 nM) with potent anti-proliferative activity.

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Filanesib, CAS 885060-09-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 243.00
50 mg	In stock	$ 397.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 98.06%

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Description	Filanesib (ARRY 520) is a selective inhibitor of kinesin spindle protein (KSP, IC50 = 6 nM) with potent anti-proliferative activity.
Targets&IC50	KSP:6 nM
In vitro	Filanesib shows anti-proliferative activity in multidrug-resistant cell lines including HCT-15, NCI/ADR-RES and K562/ADR with EC50 values of 3.7, 14 and 4.2 nM respectively. Filanesib (10 nM) blocks mitosis with the monopolar spindle structure typical of KSP inhibition as judged by both increased phosphorylation of histone H3 and the accumulation of cyclin B1 in four cells [2]. Filanesib (1 nM) induces a significant G2M cell cycle block in OCI-AML3 cells at 24 hours [4].
In vivo	Filanesib (10, 15, 20, 30 mg/kg, i.p.) is active in UISO-BCA-1 xenograft, and also superior to paclitaxel in mice bearing subcutaneous HT-29, HCT-116, MDA-MB-231 and A2780 xenografts. Filanesib is superior to docetaxel in the androgen receptor-negative prostate cancer xenograft model PC-3 [1]. RPMI 8226 tumor xenografts are particularly sensitive to low doses of Filanesib (12.5 mg/kg, i.p.) [2]. Filanesib significantly inhibits tumor growth in HL60 and MV4-11 xenografts of SCID mice at concentrations of 27 mg/kg and 20 mg/kg, respectively [4].
Cell Research	Exponentially growing cells (0.4×10^6/mL) are treated with ARRY-520 for up to 48 hours. For combination, HL-60 and HL-60Bcl-2 cells (0.4×10^6/mL) are incubated with ARRY-520, ABT-737, or both for up to 96 hours. DMSO is used as the control agent. Apoptosis is estimated by flow cytometry measurements of phosphatidylserine with the Annexin-V-FLUOS Staining Kit. Membrane integrity is simultaneously assessed by 7-amino-actinomycin D (7-AAD). To measure changes in the mitochondrial membrane potential (MMP), cells are loaded with CMXRos (300 nM) and MitoTracker Green (500 nM) for 1 hour at 37°C. The loss of MMP is then assessed by measuring CMXRos retention while simultaneously adjusting for mitochondrial mass [4].
Animal Research	Subcutaneous tumor xenografts are allowed to grow to a volume of 250-350 mm3. The mice are randomized into groups of 3-4 based on tumor size and are given a single dose of ARRY-520 i.p. At various time-points after administration of the drug, the mice are euthanized by CO2 inhalation and the tumors excised and placed in 10% neutral buffered formalin. The formalin-fixed tumors are processed and paraffin-embedded by standard procedures. Spindle morphology is analyzed by staining tumor sections for α-tubulin, and apoptosis is analyzed by TUNEL stain. Monopolar/abnormal spindles and TUNEL positive (apoptotic) cells are counted in three ×40 fields from each sample, analyzed using algorithms developed in software [1].

Synonyms	ARRY-520, ARRY 520
Molecular Weight	420.48
Formula	C20H22F2N4O2S
CAS No.	885060-09-3

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/mL (214 mM)

References and Literature

1. Woessner R, et al. ARRY-520, a novel KSP inhibitor with potent activity in hematological and taxane-resistant tumor models. Anticancer Res. 2009 Nov;29(11):4373-80. 2. Tunquist BJ, et al. Mcl-1 stability determines mitotic cell fate of human multiple myeloma tumor cells treated with the kinesin spindle protein inhibitor ARRY-520. Mol Cancer Ther. 2010 Jul;9(7):2046-56. 3. Kim KH, et al. KSP inhibitor ARRY-520 as a substitute for Paclitaxel in Type I ovarian cancer cells. J Transl Med. 2009 Jul 20;7:63. 4. Carter BZ, et al. Inhibition of KSP by ARRY-520 induces cell cycle block and cell death via the mitochondrial pathway in AML cells. Leukemia. 2009 Oct;23(10):1755-62.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Drug Library Bioactive Compound Library Clinical Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library

Related Products

Related compounds with same targets

ARRY 520 hydrochloride SB-743921 hydrochloride Ispinesib

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Keywords

Filanesib 885060-09-3 Cell Cycle/Checkpoint KSP ARRY-520 ARRY520 ARRY 520 inhibitor inhibit

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