Filanesib TFA

Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib TFA induces cell death by apoptosis in vitro. Filanesib TFA has potent anti-proliferative activity.

Product information

CAS Number: 1781834-99-8

Molecular Weight: 534.50

Formula: C22H23F5N4O4S

Chemical Name: (2S)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-2,3-dihydro-1,3,4-thiadiazole-3-carboxamide; trifluoroacetic acid

Smiles: CN(OC)C(=O)N1N=C(S[C@@]1(CCCN)C1C=CC=CC=1)C1=CC(F)=CC=C1F.OC(=O)C(F)(F)F

InChiKey: CIJUJPVFECBUKG-BDQAORGHSA-N

InChi: InChI=1S/C20H22F2N4O2S.C2HF3O2/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;3-2(4,5)1(6)7/h3-5,7-10,13H,6,11-12,23H2,1-2H3;(H,6,7)/t20-;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Filanesib TFA inhibits human KSP with an IC50 of 6 nM by a mechanism demonstrated to be uncompetitive with respect to ATP and noncompetitive with respect to tubulin. Filanesib TFA induces mitotic arrest in multiple cell lines. Filanesib TFA exhibits anti-proliferative against a broad range of human and rodent tumor cell lines. Filanesib TFA (0.001-0.1 nM; 36 hours) induces apoptosis, by a mechanism that is independent of p53 status, as defined by formation of nucleosomes and activation of caspases 3 and 7, as well as accumulation in SubG0/1 by FACS . Filanesib TFA (0.1-100 nM; 18 hours) induces the accumulation of phospho-Histone H3 (a marker of mitosis, and an indicator of mitotic arrest) in HeLa cells. Filanesib TFA (0.78-6.25 nM; 44 hours) treatment results in G2/M arrest. Filanesib TFA (10 nM; 16 hours) treatment results in the formation of monopolar spindles. Filanesib TFA potently induces cell cycle block and subsequent death in leukemic cells via the mitochondrial pathway and has potential to eradicate AML progenitor cells. Filanesib TFA (3 μM; 6-24 hours) is able to induce caspase-2 activation. Filanesib TFA (0.003-3 μM; 24-48 hours) is cytotoxic in Type II EOC cells.

In Vivo:

Filanesib TFA (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo.

Products are for research use only. Not for human use.