ARRY-520 (trifluoroacetate salt)
- CAS No.
- 1781834-99-8
- Chemical Name:
- ARRY-520 (trifluoroacetate salt)
- Synonyms
- ARRY520 TFA;ARRY 520 TFA;ARRY-520 TFA;Filanesib TFA;Filanesib trifluoroacetic acid;ARRY-520 (trifluoroacetate salt)
- CBNumber:
- CB94666047
- Molecular Formula:
- C22H23F5N4O4S
- Molecular Weight:
- 534.5
- MDL Number:
- MFCD23381173
- MOL File:
- 1781834-99-8.mol
ARRY-520 (trifluoroacetate salt) Chemical Properties,Uses,Production
Description
Filanesib, also known as ARRY-520, is a synthetic, small molecule targeting the kinesin spindle protein (KSP) with potential antineoplastic activity. KSP inhibitor ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during the mitotic phase, and consequently cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neuronal transport, this agent does not cause the peripheral neuropathy that is often associated with tubulin-targeting agents.
in vitro
Inhibition of KSP by ARRY-520 blocked cell cycle progression, leading to apoptosis in acute myeloid leukemia cell lines that express high levels of KSP. Knockdown of p53, overexpression of XIAP and mutation in caspase-8 did not significantly affect sensitivity to ARRY-520, suggesting that the response is independent of p53, XIAP and the extrinsic apoptotic pathway. Although ARRY-520 induced mitotic arrest in both HL-60 and Bcl-2-overexpressing HL-60Bcl-2 cells, cell death was blunted in HL-60Bcl-2 cells, suggesting that the apoptotic program is executed through the mitochondrial pathway. Furthermore, ARRY-520 increased Bim protein levels prior to caspase activation in HL-60 cells._x000D_ _x000D_ Reference: Leukemia. 2009 Oct;23(10):1755-62. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3593228/
target
Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP.
storage
Store at -20°C
ARRY-520 (trifluoroacetate salt) Preparation Products And Raw materials
Raw materials
Preparation Products
ARRY-520 (trifluoroacetate salt) Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 4249 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.com | China | 24246 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |
| Aladdin Scientific | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 58 |
| TargetMol Chemicals Inc. | 58 |