FILANESIB

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C20H22F2N4O2S
Molecular Weight	420.476
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CON(C)C(=O)N1N=C(S[C@@]1(CCCN)C2=CC=CC=C2)C3=CC(F)=CC=C3F

InChI

InChIKey=LLXISKGBWFTGEI-FQEVSTJZSA-N

InChI=1S/C20H22F2N4O2S/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/h3-5,7-10,13H,6,11-12,23H2,1-2H3/t20-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C20H22F2N4O2S
Molecular Weight	420.476
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.arraybiopharma.com/product-pipeline/filanesib/
Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800026254

Filanesib is a highly selective, targeted KSP inhibitor with a mechanism of action distinct from currently available myeloma therapies such as immunomodulatory drugs (IMiDs®) and proteasome inhibitors. Across multiple studies, filanesib has demonstrated activity in heavily pretreated multiple myeloma patients, with a consistent safety profile including no drug-induced peripheral neuropathy and limited non-hematologic toxicity. Adverse events are generally limited to transient, non-cumulative and predominantly asymptomatic myelosuppression (decreases in blood counts) when supportive measures are used. Alpha 1-acid glycoprotein (AAG), a plasma protein, is a potential patient selection marker for filanesib. AAG is undergoing further investigation in clinical trials and could represent the first patient selection marker for a myeloma therapy. Filanesib is in Phase II for Multiple myeloma treatment.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Kinesin-like protein 1 12 Target ID: CHEMBL4581 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26396688	Inhibitor 8504		18.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Multiple myeloma 159 Sources: http://adisinsight.springer.com/drugs/800026254	Primary		Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
72 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25684345	2.5 mg/m² single, intravenous dose: 2.5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:		FILANESIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
1570 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25684345	2.5 mg/m² single, intravenous dose: 2.5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:		FILANESIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
66 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25684345	2.5 mg/m² single, intravenous dose: 2.5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:		FILANESIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252	inhibitor 2438	inhibitor 2507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1741

Drug as perpetrator

Target	Modality	Activity
P-gp 1932	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1346987#sid=363679166	yes [IC50 0.1636 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1645841#sid=363679166	yes [IC50 1.5092 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1645841#sid=363679166	yes [IC50 18.9991 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1645841#sid=363679166	yes [IC50 3.0112 uM]

Sourcing

Vendor/Aggregator	ID	URL
1PlusChem LLC	1P00GUHM	https://www.1pchem.com/search?query=1P00GUHM
1PlusChem LLC	1P00GUHN	https://www.1pchem.com/search?query=1P00GUHN
AChemBlock	F-4326	http://www.achemblock.com/catalogsearch/result/?q=F-4326
AK Scientific	3452AH	https://aksci.com/item_detail.php?cat=3452AH
ApexBio Technology	A3188	https://www.apexbt.com/catalogsearch/result/?q=A3188
ApexBio Technology	A4458	https://www.apexbt.com/catalogsearch/result/?q=A4458
BLD Pharm	BD630958	http://www.bldpharm.com/search/Search.html?keyword=BD630958
BOC Sciences	885060-09-3	http://www.bocsci.com/description.asp?cas=885060-09-3
Cayman Chemical	21883	http://www.caymanchem.com/app/template/Product.vm/catalog/21883
Chem Scene	CS-0867	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0867
ChemShuttle	169457	https://www.chemshuttle.com/catalogsearch/result/?q=169457
eMolecules	193590738	https://orderbb.emolecules.com/search/#?query=193590738
eMolecules	300567880	https://orderbb.emolecules.com/search/#?query=300567880
eMolecules	44786317	https://orderbb.emolecules.com/search/#?query=44786317
eMolecules	44811470	https://orderbb.emolecules.com/search/#?query=44811470
Excenen	EX-A678	http://www.excenen.com/searchresultlist.php?id=EX-A678
mcule	MCULE-6516697262	https://mcule.com/MCULE-6516697262/
mcule	MCULE-9374698438	https://mcule.com/MCULE-9374698438/
MedChem Express	HY-15187	https://www.medchemexpress.com/search.html?q=HY-15187&ft=&fa=&fp=
MolPort	MolPort-028-720-385	https://www.molport.com/shop/molecule-link/MolPort-028-720-385
MolPort	MolPort-035-765-791	https://www.molport.com/shop/molecule-link/MolPort-035-765-791
MolPort	MolPort-039-139-554	https://www.molport.com/shop/molecule-link/MolPort-039-139-554
MuseChem	M143312	https://www.musechem.com/product/M143312.html
ShangHai Biochempartner	BCP07442	http://www.biochempartner.com/search_BCP07442
Tocris	4676	https://www.tocris.com/search.php?Type=QuickSearch&Value=4676
Toronto Research Chemicals	A628325	https://www.trc-canada.com/product-detail/?CatNum=A628325
Toronto Research Chemicals	D229675	https://www.trc-canada.com/product-detail/?CatNum=D229675

PubMed

Title	Date	PubMed
Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent.	2011-10-13	21899292

Patents

Sample Use Guides

In Vivo Use Guide

intravenously either at a dose of 1.5 mg/m2 /day (schedule 1: days 1, 2, 15, and 16) or 3 mg/m2 /day (schedule 2: days 1 and 15).

Route of Administration: Intravenous

In Vitro Use Guide

Filanesib inhibited His-tagged KSP motor domain assessed as inhibition of microtubule-stimulated KSP ATPase activity with IC50 18nM

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:04:17 GMT 2025` Edited by `admin` on `Mon Mar 31 18:04:17 GMT 2025`
Record UNII	8A49OSO368
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

FILANESIB

Official Name

English

ARRY-520

Preferred Name

English

FILANESIB [USAN]

Common Name

English

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

Systematic Name

English

1,3,4-THIADIAZOLE-3(2H)-CARBOXAMIDE, 2-(3-AMINOPROPYL)-5-(2,5-DIFLUOROPHENYL)-N-METHOXY-N-METHYL-2-PHENYL-, (2S)-

Systematic Name

English

filanesib [INN]

Common Name

English

Filanesib [WHO-DD]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C67440