ARRY 520 trifluoroacetate ((2S)-2-(3-Aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3(2H)-carboxamide trifluoroacetate) | 885060-09-3

name

arry 520 trifluoroacetate

chemical name

(2s)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-n-methoxy-n-methyl-2-phenyl-1,3,4-thiadiazole-3(2h)-carboxamide trifluoroacetate

activity

potent kinesin spindle protein (ksp) inhibitor (ic50 = 6 nm); selective for ksp over >250 other receptors and kinases at a concentration of 10 μm. displays robust antitumor activity in bortezomib-resistant xenografts either alone or in combination with bortezomib. induces degradation of mcl-1; exhibits comparable cytotoxic activity to taxol (cat. no. 1097) in epithelial ovarian cancer cells. active in vivo.

MW

420.48

Formula:

c20h22f2n4o2s.cf3co2h

Solubility:

soluble to 75 mm in dmso and to 75 mm in ethanol

Purity:

>98 %

Storage:

store at -20°c

CAS No:

885060-09-3

Kim et al (2009) KSP inhibitor ARRY-520 as a substitute for Paclitaxel in type I ovarian cancer cells. J.Transl.Med. 7 63. PMID: 19619321.

Woessner et al (2009) ARRY-520, a novel KSP inhibitor with potent activity in hematological and taxane-resistant tumor models. Anticancer Res. 29 4373. PMID: 20032381.

Tunquist et al (2010) 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. 9 2046. PMID: 20571074.