ARRY-520

• CAT Number: I005313
• CAS Number: 885060-09-3
• Molecular Formula: C20H22F2N4O2S
• Molecular Weight: 420.5
• 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

ARRY-520 (Cat.No:I005313) is a small molecule drug that acts as a kinesin spindle protein (KSP) inhibitor. It has shown promise as a treatment for multiple myeloma and other hematologic malignancies. ARRY-520 inhibits cell division by blocking the assembly of microtubules, which are essential for cell division. Clinical trials have demonstrated the safety and efficacy of ARRY-520 in treating multiple myeloma.

Reference

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 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 Article3: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 Article4: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 Article5: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 Article6: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