[CAS NO. 885060-09-3] Filanesib

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PRODUCTS SPECIFICATIONS [885060-09-3]

Catalog

HY-15187

Brand

MCE

CAS

885060-09-3

DESCRIPTION [885060-09-3]

Overview

MDL	MFCD18633235
Molecular Weight	420.48
Molecular Formula	C20H22F2N4O2S
SMILES	O=C(N1[C@@](C2=CC=CC=C2)(CCCN)SC(C3=CC(F)=CC=C3F)=N1)N(OC)C

For research use only. We do not sell to patients.

3 Publications Citing Use of MCE

Summary

Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein ( KSP ) inhibitor, with an IC ₅₀ of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity ^[1] .

IC50 & Target

KSP

6 nM (IC ₅₀ )

In Vitro

Filanesib induces mitotic arrest in multiple cell lines ^[1] .
Filanesib exhibits anti-proliferative against a broad range of human and rodent tumor cell lines, including a variety of leukemias and solid tumors, with EC ₅₀ s between 0.4 nM and 14.4 nM ^[1] .
Filanesib (0.001-0.1 nM; 36 hours) induces apoptosis in a dose-dependent manner in HeLa cells ^[1] .
Filanesib (3.13-6.25 nM; 44 hours) causes accumulation of cells in the G2/M phase of the cell cycle in a dose-dependent manner in HeLa cells ^[1] .
Filanesib potently induces cell cycle block and subsequent death in leukemic cells via the mitochondrial pathway and has potential to eradicate AML progenitor cells ^[2] .
Filanesib (3 μM; 6-24 hours) is able to induce caspase-2 activation ^[3] .
Filanesib (0.003-3 μM; 24-48 hours) is cytotoxic in Type II EOC cells ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis ^[1]

Cell Line:	Hela cells
Concentration:	0.01-0.1 nM
Incubation Time:	36 hours
Result:	Induced the formation of nucleosomes and activation of caspases-3 and 7.

Cell Cycle Analysis ^[1]

Cell Line:	HeLa cells
Concentration:	0.78 nM, 1.56 nM, 3.13 nM, 6.25 nM
Incubation Time:	44 hours
Result:	Resulted in G2/M arrest.

Western Blot Analysis ^[3]

Cell Line:	Type II EOC cells
Concentration:	3 μM
Incubation Time:	6 hours, 12 hours, 24 hours
Result:	Induced caspase-2 activation in a time-dependent manner.

Cell Cytotoxicity Assay ^[3]

Cell Line:	Type II EOC cell lines (A2780, CP70, 01-28)
Concentration:	0.003 μM, 0.03 μM, 0.3μM, 3 μM
Incubation Time:	24 hours , 48 hours
Result:	Effectively decreased cell viability in a time-dependent manner in the Type II EOC cell lines.

In Vivo

Filanesib (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nude mice, EOC mice xenograft model ^[3]
Dosage:	20 mg/kg, 30 mg/kg
Administration:	Intraperitoneal injection, q4dx3
Result:	Induced a decrease in tumor kinetics in a dose-dependent manner.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01372540	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Plasma Cell Leukemia\|Recurrent Plasma Cell Myeloma\|Refractory Plasma Cell Myeloma	February 24, 2012	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 237.82 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3782 mL	11.8912 mL	23.7823 mL
5 mM	0.4756 mL	2.3782 mL	4.7565 mL
10 mM	0.2378 mL	1.1891 mL	2.3782 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

1,3,4-Thiadiazole-3(2H)-carboxamide, 2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-, (2S)-

(2S)-2-(3-Aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3(2H)-carboxamide

Filanesib

ARRY 520

(2S)-2-(3-Aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3-carboxamide