BMS-214662

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C25H23N5O2S2
Molecular Weight	489.612
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O=S(=O)(N1CC2=CC(=CC=C2N(CC3=CN=CN3)C[C@H]1CC4=CC=CC=C4)C#N)C5=CC=CS5

InChI

InChIKey=OLCWFLWEHWLBTO-HSZRJFAPSA-N

InChI=1S/C25H23N5O2S2/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/h1-11,14,18,23H,12,15-17H2,(H,27,28)/t23-/m1/s1

HIDE SMILES / InChI

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 8504		0.7 nM [IC50]

PubMed

Title	Date	PubMed
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.	2010-09	21695007
Farnesyltransferase inhibitor BMS-214662 induces apoptosis in myeloma cells through PUMA up-regulation, Bax and Bak activation, and Mcl-1 elimination.	2005-06	15738311
Targeting RAS signalling pathways in cancer therapy.	2003-01	12509763
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.	2000-10-05	11020273

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 `Mon Mar 31 19:00:20 GMT 2025` Edited by `admin` on `Mon Mar 31 19:00:20 GMT 2025`
Record UNII	L2U9GFD244
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BMS-214662

Code

English

BMS 214662

Preferred Name

English

(R)-2,3,4,5-TETRAHYDRO-1-(1H-IMIDAZOL-4-YLMETHYL)-3-(PHENYLMETHYL)-4-(2-THIENYLSULFONYL)-1H-1,4-BENZODIAZEPINE-7-CARBONITRILE

Systematic Name

English

1H-1,4-BENZODIAZEPINE-7-CARBONITRILE, 2,3,4,5-TETRAHYDRO-1-(1H-IMIDAZOL-4-YLMETHYL)-3-(PHENYLMETHYL)-4-(2-THIENYLSULFONYL)-, (R)-

Systematic Name

English

1H-1,4-BENZODIAZEPINE-7-CARBONITRILE, 2,3,4,5-TETRAHYDRO-1-(1H-IMIDAZOL-4-YLMETHYL)-3-(PHENYLMETHYL)-4-(2-THIENYLSULFONYL)-, (3R)-

Systematic Name

English

BMS 214662 [WHO-DD]

Code

English

7-CYANO-2,3,4,5-TETRAHYDRO-1-(1H-IMIDAZOL-4-YLMETHYL)-3-(PHENYLMETHYL)-4-(2-THIENYLSULFONYL)-1H-1,4-BENZODIAZEPINE

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C2020