BMS-214662 MESYLATE

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C25H23N5O2S2.CH4O3S
Molecular Weight	585.718
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CS(O)(=O)=O.O=S(=O)(N1CC2=C(C=CC(=C2)C#N)N(CC3=CN=CN3)C[C@H]1CC4=CC=CC=C4)C5=CC=CS5

InChI

InChIKey=GQZSWQUMYWWKTN-GNAFDRTKSA-N

InChI=1S/C25H23N5O2S2.CH4O3S/c26-13-20-8-9-24-21(11-20)15-30(34(31,32)25-7-4-10-33-25)23(12-19-5-2-1-3-6-19)17-29(24)16-22-14-27-18-28-22;1-5(2,3)4/h1-11,14,18,23H,12,15-17H2,(H,27,28);1H3,(H,2,3,4)/t23-;/m1./s1

HIDE SMILES / InChI

Molecular Formula	CH4O3S
Molecular Weight	96.106
Charge	0
Count

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

Molecular Formula	C25H23N5O2S2
Molecular Weight	489.612
Charge	0
Count

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12789624 | https://adisinsight.springer.com/drugs/800013625

Bristol-Myers Squibb developed BMS-214662 as potent and selective farnesyl transferase inhibitor with potent antitumor activity. BMS-214662 participated in phase II trials in the US for pancreatic, head and neck, lung and colorectal cancers. However, further information is not available.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Protein farnesyltransferase 13 Target ID: CHEMBL2094108 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14741286	Inhibitor 8297		0.7 nM [IC50]

PubMed

Title	Date	PubMed
Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.	2000 Oct 5	11020273
Targeting RAS signalling pathways in cancer therapy.	2003 Jan	12509763
Farnesyltransferase inhibitor BMS-214662 induces apoptosis in myeloma cells through PUMA up-regulation, Bax and Bak activation, and Mcl-1 elimination.	2005 Jun	15738311
Design, Synthesis and Evaluation of Novel 1-(Substituted Acetyl)-4-(10-Bromo-8-Chloro-5,6-Dihydro-11H-Benzo[5,6]Cyclohepta[1,2-B]Pyridine-11-Ylidene)piperidines as Antitumor Agents and Farnesyl Protein Transferase Inhibitors.	2010 Sep	21695007

Patents

Sample Use Guides

In Vivo Use Guide

Patients were treated every week as tolerated with i.v. paclitaxel (fixed dose, 80 mg/m(2)/wk) administered over 1 h followed by i.v. BMS-214662 (escalating doses, 80-245 mg/m(2)/wk) over 1 h starting 30 min after completion of paclitaxel.

Route of Administration: Intravenous

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:47:48 UTC 2023` Edited by `admin` on `Fri Dec 15 15:47:48 UTC 2023`
Record UNII	CY68RYB4QI
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BMS-214662 MESYLATE

Common Name

English

Code System Code Type Description

PUBCHEM

72941825

Created by admin on Fri Dec 15 15:47:48 UTC 2023 , Edited by admin on Fri Dec 15 15:47:48 UTC 2023

PRIMARY

DRUG BANK

DBSALT002162

Created by admin on Fri Dec 15 15:47:48 UTC 2023 , Edited by admin on Fri Dec 15 15:47:48 UTC 2023

PRIMARY

FDA UNII

CY68RYB4QI

Created by admin on Fri Dec 15 15:47:48 UTC 2023 , Edited by admin on Fri Dec 15 15:47:48 UTC 2023

PRIMARY

CAS

474010-58-7

Created by admin on Fri Dec 15 15:47:48 UTC 2023 , Edited by admin on Fri Dec 15 15:47:48 UTC 2023

PRIMARY

Details

SMILES

InChI

DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/12789624 | https://adisinsight.springer.com/drugs/800013625

Originator

Approval Year

Targets

PubMed

Patents

Sample Use Guides

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12789624 | https://adisinsight.springer.com/drugs/800013625