885060-09-3

Basic information

• Product Name: ARRY-520
• Synonyms: (2S)-2-(3-Aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3(2H)-carboxamide;Filanesib;1,3,4-Thiadiazole-3(2H)-carboxamide, 2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-, (2S)-;Arry-520 (Filanesib);Finerenone;ARRY-520
• CAS NO: 885060-09-3
• Molecular Formula: C20H22F2N4O2S
• Molecular Weight: 420.4760864
• Mol File: 885060-09-3.mol

Chemical Properties

• Boiling Point: 511.3±60.0 °C(Predicted)
• Appearance: /
• Density: 1.31±0.1 g/cm3(Predicted)
• Solubility: Soluble in DMSO
• PKA: 10.10±0.10(Predicted)
• CAS DataBase Reference: ARRY-520(CAS DataBase Reference)
• NIST Chemistry Reference: ARRY-520(885060-09-3)
• EPA Substance Registry System: ARRY-520(885060-09-3)

Safety Data

• Hazardous Substances Data: 885060-09-3(Hazardous Substances Data)

Usage

Uses

Used in Oncology:
ARRY-520 is used as an anticancer agent for the treatment of various solid tumors. It inhibits the kinesin spindle protein, which is essential for the formation and function of the mitotic spindle during cell division. This leads to cell cycle arrest in the mitotic phase and subsequent apoptosis, resulting in the inhibition of tumor growth and progression.
Used in Drug Development:
ARRY-520 serves as a valuable compound in the development of new cancer therapies. Its potent inhibitory activity against kinesin spindle protein makes it a promising candidate for further research and development as a targeted cancer treatment. Additionally, its mechanism of action can be studied to identify potential synergistic effects with other anticancer agents, enhancing the overall efficacy of combination therapies.

Biological Activity

arry 520 trifluoroacetate is a synthetic and salt form of ksp inhibitor with ic50 value of 6 nm.kinesin spindle protein (ksp) is one member of the mitotic kinesins involved in the early stages of mitosis responsible for centrosome separation.

in vitro

arry-520 had low nanomolar antiproliferative activity in various tumor cell lines and exhibited activity in multidrug-resistant cell lines. ec50s of arry-520 for proliferation inhibition in hct-15, nci/adr-res and k562/adr cells was 3.7, 14 and 4.2 nm, respectively, while paclitaxel ec50s in these cell lines was 35, 565 and 372 nm. moreover, k562/adr was found to be 118-fold resistant to paclitaxel when compared to the parent k562 line, but only 3.5-fold resistant to that of arry-520 [1].

in vivo

arry-520 was found to be active in uiso-bca-1 xenografts, which were completely resistant to paclitaxel. the antitumor efficacy of arry-520 was also found to be superior to paclitaxel in mice bearing ht-29, hct-116, mda-mb-231 and a2780 xenografts. arry-520 was superior to docetaxel in the androgen receptor-negative prostate cancer pc-3 xenograft model, and was also superior to docetaxel in the du145 prostate xenograft model [1].