SNS-032

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C17H24N4O2S2
Molecular Weight	380.528
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)(C)C1=CN=C(CSC2=CN=C(NC(=O)C3CCNCC3)S2)O1

InChI

InChIKey=OUSFTKFNBAZUKL-UHFFFAOYSA-N

InChI=1S/C17H24N4O2S2/c1-17(2,3)12-8-19-13(23-12)10-24-14-9-20-16(25-14)21-15(22)11-4-6-18-7-5-11/h8-9,11,18H,4-7,10H2,1-3H3,(H,20,21,22)

HIDE SMILES / InChI

Molecular Formula	C17H24N4O2S2
Molecular Weight	380.528
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19169685 | https://www.ncbi.nlm.nih.gov/pubmed/15027863 | http://adisinsight.springer.com/drugs/800016657 | https://www.ncbi.nlm.nih.gov/pubmed/17938863

SNS-032 (formerly BMS-387032) is a potent, selective inhibitor of cyclin-dependent kinases (CDK). SNS-032 blocks the cell cycle via inhibition of CDKs 2 and 7, and transcription via inhibition of CDKs 7 and 9. SNS-032 was investigated for the treatment of solid tumors and hematologic malignancies (Phase I studies), however, its development was discontinued.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Cyclin-dependent kinase 2/cyclin E 10 Target ID: CHEMBL2094126 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15027863	Inhibitor 8504	48.0 nM [IC50]
CDK9/cyclin T1 4 Target ID: CHEMBL2111389 Sources: https://www.sunesis.com/data-pdf/032/poster5_04_06.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/19169685	Inhibitor 8504	5.0 nM [Ki]
CDK2/Cyclin A 7 Target ID: CHEMBL3038469 Sources: https://www.sunesis.com/data-pdf/032/poster5_04_06.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/19169685	Inhibitor 8504	70.0 nM [Ki]
Cyclin-dependent kinase 7/ cyclin H 7 Target ID: CHEMBL2111288 Sources: https://www.sunesis.com/data-pdf/032/poster5_04_06.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/19169685	Inhibitor 8504	60.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Cancer 609 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17938863 http://adisinsight.springer.com/drugs/800016657	Primary		Phase I 438	Unknown Approved Use Unknown
Hematologic malignancies 19 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17938863 http://adisinsight.springer.com/drugs/800016657	Primary		Phase I 438	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
251.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20479412/	75 mg/m² 3 times / 4 weeks multiple, intravenous dose: 75 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered:	SNS-032 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.287 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17938863	16 mg/m² single, intravenous dose: 16 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SNS-032 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.017 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17938863	16 mg/m² single, oral dose: 16 mg/m² route of administration: Oral experiment type: SINGLE co-administered:	SNS-032 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
2767 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20479412/	75 mg/m² 3 times / 4 weeks multiple, intravenous dose: 75 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered:	SNS-032 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.553 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17938863	16 mg/m² single, intravenous dose: 16 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SNS-032 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.052 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17938863	16 mg/m² single, oral dose: 16 mg/m² route of administration: Oral experiment type: SINGLE co-administered:	SNS-032 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
9.02 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20479412/	75 mg/m² 3 times / 4 weeks multiple, intravenous dose: 75 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered:	SNS-032 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17938863	16 mg/m² single, intravenous dose: 16 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SNS-032 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17938863	16 mg/m² single, oral dose: 16 mg/m² route of administration: Oral experiment type: SINGLE co-administered:	SNS-032 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
37% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15027863	unknown, unknown		SNS-032 serum	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Sourcing

Vendor/Aggregator	ID	URL
1PlusChem LLC	1P00C6YD	https://www.1pchem.com/search?query=1P00C6YD
A2B Chem	AF68085	http://a2bchem.com/prod/AF68085
AChemBlock	10384	http://www.achemblock.com/catalogsearch/result/?q=10384
AK Scientific	SYN1080	https://aksci.com/item_detail.php?cat=SYN1080
AK Scientific	X7382	https://aksci.com/item_detail.php?cat=X7382
Ambeed	A153280	http://www.ambeed.com/search/Search.html?keyword=A153280
ApexBio Technology	A1980	https://www.apexbt.com/catalogsearch/result/?q=A1980
AstaTech	41327	http://astatechinc.com/CPSResult.php?CRNO=41327
Axon MedChem	1614	https://www.axonmedchem.com/product/1614
BLD Pharm	BD165410	http://www.bldpharm.com/search/Search.html?keyword=BD165410
BOC Sciences	345627-80-7	http://www.bocsci.com/description.asp?cas=345627-80-7
Capot Chemical	16670	https://www.capotchem.com/search.do?q=16670
Cayman Chemical	17904	http://www.caymanchem.com/app/template/Product.vm/catalog/17904
Chem Scene	CS-0021	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0021
ChemShuttle	109817	https://www.chemshuttle.com/catalogsearch/result/?q=109817
ChemShuttle	149126	https://www.chemshuttle.com/catalogsearch/result/?q=149126
Combi-Blocks	QJ-1343	http://www.combi-blocks.com/cgi-bin/find.cgi?QJ-1343
eMolecules	10705199	https://orderbb.emolecules.com/search/#?query=10705199
eMolecules	31507563	https://orderbb.emolecules.com/search/#?query=31507563
eMolecules	44696712	https://orderbb.emolecules.com/search/#?query=44696712
eNovation Chemicals	D320225	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D320225&searchbtn.x=0&searchbtn.y=0
eNovation Chemicals	D552382	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D552382&searchbtn.x=0&searchbtn.y=0
eNovation Chemicals	D663018	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D663018&searchbtn.x=0&searchbtn.y=0
Excenen	EX-A054	http://www.excenen.com/searchresultlist.php?id=EX-A054
Fluorochem	240573	http://www.fluorochem.co.uk/Products/Product?code=240573
Hairui	HR110690	http://www.hairuichem.com/en/product/search.do?q=HR110690
Hairui	HR121225	http://www.hairuichem.com/en/product/search.do?q=HR121225
KeyOrganics	AS-16235	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-16235
KeyOrganics	AS-35116	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-35116
Lab Network	LN01304605	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01304605
Lab Seeker	SC-84716	http://www.labseeker.com/search.php?keywords=SC-84716&category=0
LabSeeker	SC-84716	http://www.labseeker.com/search.php?keywords=SC-84716&category=0
Matrix Scientific	146701	http://www.matrixscientific.com/146701.html
mcule	MCULE-3980461563	https://mcule.com/MCULE-3980461563/
mcule	MCULE-7173755768	https://mcule.com/MCULE-7173755768/
MedChem Express	HY-10008	https://www.medchemexpress.com/search.html?q=HY-10008&ft=&fa=&fp=
Molnova	M14183	https://www.molnova.com/en/serch-list.html?keywords=M14183
MolPort	MolPort-005-942-660	https://www.molport.com/shop/molecule-link/MolPort-005-942-660
MolPort	MolPort-039-062-140	https://www.molport.com/shop/molecule-link/MolPort-039-062-140
MuseChem	I003261	https://www.musechem.com/product/I003261.html
ShangHai Biochempartner	BCP000203	http://www.biochempartner.com/search_BCP000203
ShangHai Biochempartner	BCP000355	http://www.biochempartner.com/search_BCP000355
ShangHai Biochempartner	BCP01951	http://www.biochempartner.com/search_BCP01951
ShangHai Biochempartner	BCP02418	http://www.biochempartner.com/search_BCP02418
ShangHai Biochempartner	BCP06530	http://www.biochempartner.com/search_BCP06530
TargetMol	T6049	https://www.targetmol.com/search?keyword=T6049
Tocris	4075	https://www.tocris.com/search.php?Type=QuickSearch&Value=4075
Toronto Research Chemicals	S590100	https://www.trc-canada.com/product-detail/?CatNum=S590100
W&J PharmaChem	50C1004546	http://wjpharmachem.com/new/searcht.php?keyword=50C1004546

PubMed

Title	Date	PubMed
Comprehensive analysis of kinase inhibitor selectivity.	2011-10-30	22037378
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.	2010-11-24	21095574
Responses in mantle cell lymphoma cells to SNS-032 depend on the biological context of each cell line.	2010-08-15	20663900
Phase I and pharmacologic study of SNS-032, a potent and selective Cdk2, 7, and 9 inhibitor, in patients with advanced chronic lymphocytic leukemia and multiple myeloma.	2010-06-20	20479412
The small-molecule CDK inhibitor, SNS-032, enhances cellular radiosensitivity in quiescent and hypoxic non-small cell lung cancer cells.	2009-10	19193471
SNS-032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples.	2009-09	19169685
Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia.	2009-05-07	19234140
SNS-032 prevents hypoxia-mediated glioblastoma cell invasion by inhibiting hypoxia inducible factor-1alpha expression.	2009-04	19287962
Transient treatment with CDK inhibitors eliminates proliferative potential even when their abilities to evoke apoptosis and DNA damage are blocked.	2008-12-15	19066469
Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.	2008-12-01	18926699
A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.	2008-11-01	18842409
A phase 1 study of SNS-032 (formerly BMS-387032), a potent inhibitor of cyclin-dependent kinases 2, 7 and 9 administered as a single oral dose and weekly infusion in patients with metastatic refractory solid tumors.	2008-02	17938863
Transcriptional upregulation of p57 (Kip2) by the cyclin-dependent kinase inhibitor BMS-387032 is E2F dependent and serves as a negative feedback loop limiting cytotoxicity.	2007-05-24	17173074
SNS-032 prevents tumor cell-induced angiogenesis by inhibiting vascular endothelial growth factor.	2007-05	17534442
Drugging cell cycle kinases in cancer therapy.	2005-05	15857291
P-glycoprotein plays a role in the oral absorption of BMS-387032, a potent cyclin-dependent kinase 2 inhibitor, in rats.	2005-02	15338193
E2F4 deficiency promotes drug-induced apoptosis.	2004-12	15611646
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.	2004-03-25	15027863

Patents

Sample Use Guides

In Vivo Use Guide

Patients with metastatic solid tumors or refractory lymphoma were treated with a starting dose of 4 mg/m2 intravenously administered over 1-h with a cycle defined as 3 weekly doses of SNS-032 every 21 days. Three patient cohorts were utilized in the dose-escalation schema. Pharmacokinetic studies were performed. For the 13 and 16 mg/m2 dose cohorts, the first dose of cycle 2 was given as an oral solution to estimate the oral bioavailability of the drug in humans.

Route of Administration: Other

In Vitro Use Guide

Treatment of RPMI-8226 MM cells with 300 nM SNS-032 (IC(90)) for 6 h was sufficient for commitment to apoptosis. Antiproliferative activity was established in an A2780 cellular cytotoxicity assay in which SNS-032 showed an IC(50) = 95 nM.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 19:44:06 GMT 2025` Edited by `admin` on `Mon Mar 31 19:44:06 GMT 2025`
Record UNII	9979I93686
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

BMS-387032

Preferred Name

English

SNS-032

Common Name

English

BMS387032

Common Name

English

N-(5-(((5-(1,1-DIMETHYLETHYL)-2-OXAZOLYL)METHYL)THIO)-2-THIAZOLYL)-4-PERIDINECARBOXAM

Common Name

English

SNS 032 [WHO-DD]

Common Name

English

4-PIPERIDINECARBOXAMIDE, N-(5-(((5-(1,1-DIMETHYLETHYL)-2-OXAZOLYL)METHYL)THIO)-2-THIAZOLYL)-

Systematic Name

English

Code System Code Type Description

FDA UNII

9979I93686