For research use only, not for therapeutic use.
ARRY-520 (Cat No.:I005313) is a selective kinesin spindle protein (KSP) inhibitor, which interferes with the mitotic spindle formation crucial for cell division. By targeting KSP, ARRY-520 halts mitosis and induces apoptosis in rapidly dividing cancer cells, particularly those in hematologic malignancies like multiple myeloma. Unlike traditional chemotherapies, ARRY-520 does not affect non-dividing cells, offering a more targeted approach with reduced toxicity. It has shown promising results in clinical trials, especially in patients resistant to other therapies. ARRY-520 is actively studied for its potential in advancing cancer treatment strategies.
| Catalog Number | I005313 |
| CAS Number | 885060-09-3 |
| Synonyms | (2S)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3-carboxamide |
| Molecular Formula | C20H22F2N4O2S |
| Purity | ≥95% |
| Target | Ksp |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| IC50 | 6 nM |
| IUPAC Name | (2S)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3-carboxamide |
| InChI | InChI=1S/C20H22F2N4O2S/c1-25(28-2)19(27)26-20(11-6-12-23,14-7-4-3-5-8-14)29-18(24-26)16-13-15(21)9-10-17(16)22/h3-5,7-10,13H,6,11-12,23H2,1-2H3/t20-/m0/s1 |
| InChIKey | LLXISKGBWFTGEI-FQEVSTJZSA-N |
| SMILES | CN(C(=O)N1[C@](SC(=N1)C2=C(C=CC(=C2)F)F)(CCCN)C3=CC=CC=C3)OC |
| Reference | </br>1:First-in-human phase 1 study of filanesib (ARRY-520), a kinesin spindle protein inhibitor, in patients with advanced solid tumors. LoRusso PM, Goncalves PH, Casetta L, Carter JA, Litwiler K, Roseberry D, Rush S, Schreiber J, Simmons HM, Ptaszynski M, Sausville EA.Invest New Drugs. 2015 Apr;33(2):440-9. doi: 10.1007/s10637-015-0211-0. Epub 2015 Feb 17. PMID: 25684345 </br>2:A phase 1 dose-escalation study of ARRY-520, a kinesin spindle protein inhibitor, in patients with advanced myeloid leukemias. Khoury HJ, Garcia-Manero G, Borthakur G, Kadia T, Foudray MC, Arellano M, Langston A, Bethelmie-Bryan B, Rush S, Litwiler K, Karan S, Simmons H, Marcus AI, Ptaszynski M, Kantarjian H.Cancer. 2012 Jul 15;118(14):3556-64. doi: 10.1002/cncr.26664. Epub 2011 Dec 2. PMID: 22139909 Free PMC Article</br>3:Mcl-1 stability determines mitotic cell fate of human multiple myeloma tumor cells treated with the kinesin spindle protein inhibitor ARRY-520. Tunquist BJ, Woessner RD, Walker DH.Mol Cancer Ther. 2010 Jul;9(7):2046-56. doi: 10.1158/1535-7163.MCT-10-0033. Epub 2010 Jun 22. PMID: 20571074 Free Article</br>4:ARRY-520, a novel KSP inhibitor with potent activity in hematological and taxane-resistant tumor models. Woessner R, Tunquist B, Lemieux C, Chlipala E, Jackinsky S, Dewolf W Jr, Voegtli W, Cox A, Rana S, Lee P, Walker D.Anticancer Res. 2009 Nov;29(11):4373-80. PMID: 20032381 Free Article</br>5:KSP inhibitor ARRY-520 as a substitute for Paclitaxel in Type I ovarian cancer cells. Kim KH, Xie Y, Tytler EM, Woessner R, Mor G, Alvero AB.J Transl Med. 2009 Jul 20;7:63. doi: 10.1186/1479-5876-7-63. PMID: 19619321 Free PMC Article</br>6:Inhibition of KSP by ARRY-520 induces cell cycle block and cell death via the mitochondrial pathway in AML cells. Carter BZ, Mak DH, Woessner R, Gross S, Schober WD, Estrov Z, Kantarjian H, Andreeff M.Leukemia. 2009 Oct;23(10):1755-62. doi: 10.1038/leu.2009.101. Epub 2009 May 21. PMID: 19458629 Free PMC Article |
