ARRY 520, Inhibitor | ARRY520, inhibitor

ARRY 520

Cat. Num. AAA5764565

• Purity: 98.00%
• Synonyms: ARRY 520; Filanesib; ARRY520; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 95mg/mL (225.93mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C20H22F2N4O2S
• SMILES: CN(C(=O)N1C(SC(=N1)C2=C(C=CC(=C2)F)F)(CCCN)C3=CC=CC=C3)OC
• CAS Number: 885060-09-3
• Cell Research: Exponentially growing cells (0.4x10^6/mL) are treated with ARRY-520 for up to 48 hours. For combination, HL-60 and HL-60Bcl-2 cells (0.4x10^6/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 (300nM) and MitoTracker Green (500nM) for 1 hour at 37 degree C. The loss ofmMP is then assessed by measuring CMXRos retention while simultaneously adjusting for mitochondrial mass [4].
• In Vitro: ARRY-520 (10, 15, 20, 30mg/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. ARRY-520 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 ARRY-520 (12.5mg/kg, i.p.) [2]. ARRY-520 significantly inhibits tumor growth in HL60 and MV4-11 xenografts of SCID mice at concentrations of 27mg/kg and 20mg/kg, respectively [4].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Related Product Information for ARRY520, inhibitor

ARRY-520 (Filanesib) is a synthetic kinesin spindle protein (KSP) inhibitor (IC50: 6nM).

Product Categories/Family for ARRY520, inhibitor

Cell Cycle/Checkpoint; KSP

References

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.
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.
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.
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.
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.
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.
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.
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.