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195987-41-8,MFCD09955166
Catalog No.:AA00ABU7

195987-41-8 | Bms-214662

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1mg
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00ABU7
Chemical Name:
Bms-214662
CAS Number:
195987-41-8
Molecular Formula:
C25H23N5O2S2
Molecular Weight:
489.6124
MDL Number:
MFCD09955166
SMILES:
N#Cc1ccc2c(c1)CN([C@@H](CN2Cc1[nH]cnc1)Cc1ccccc1)S(=O)(=O)c1cccs1
Properties
Computed Properties
 
Complexity:
834  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
1  
Heavy Atom Count:
34  
Hydrogen Bond Acceptor Count:
7  
Hydrogen Bond Donor Count:
1  
Rotatable Bond Count:
6  
XLogP3:
3.9  

Literature

Title: Synthesis and biological evaluation of new phenothiazine derivatives bearing a pyrazole unit as protein farnesyltransferase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20121115

Title: Modulation of anthracycline-induced cytotoxicity by targeting the prenylated proteome in myeloid leukemia cells.

Journal: Journal of molecular medicine (Berlin, Germany) 20120201

Title: The MEK inhibitor PD184352 enhances BMS-214662-induced apoptosis in CD34+ CML stem/progenitor cells.

Journal: Leukemia 20110701

Title: Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.

Journal: Journal of medicinal chemistry 20101014

Title: Novel therapeutic agents against cancer stem cells of chronic myeloid leukemia.

Journal: Anti-cancer agents in medicinal chemistry 20100201

Title: 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.

Journal: Indian journal of pharmaceutical sciences 20100101

Title: BMS-214662 induces mitochondrial apoptosis in chronic myeloid leukemia (CML) stem/progenitor cells, including CD34+38- cells, through activation of protein kinase Cbeta.

Journal: Blood 20091105

Title: Analysis of the eukaryotic prenylome by isoprenoid affinity tagging.

Journal: Nature chemical biology 20090401

Title: Chronic myelogenous leukemia stem cells: What's new?

Journal: Current hematologic malignancy reports 20090401

Title: Ethyl methanesulphonate in a parenteral formulation of BMS-214662 mesylate, a selective farnesyltransferase inhibitor: formation and rate of hydrolysis.

Journal: Pharmaceutical development and technology 20090101

Title: BMS-214662 potently induces apoptosis of chronic myeloid leukemia stem and progenitor cells and synergizes with tyrosine kinase inhibitors.

Journal: Blood 20080301

Title: Characterization of cancer stem cells in chronic myeloid leukaemia.

Journal: Biochemical Society transactions 20071101

Title: Phase I trial of weekly paclitaxel and BMS-214662 in patients with advanced solid tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070615

Title: Phase I clinical trial of the farnesyltransferase inhibitor BMS-214662 administered as a weekly 24 h continuous intravenous infusion in patients with advanced solid tumors.

Journal: Cancer chemotherapy and pharmacology 20060701

Title: Group IVC cytosolic phospholipase A2gamma is farnesylated and palmitoylated in mammalian cells.

Journal: Journal of lipid research 20051001

Title: Development of farnesyl transferase inhibitors: a review.

Journal: The oncologist 20050901

Title: Farnesyltransferase inhibitor BMS-214662 induces apoptosis in myeloma cells through PUMA up-regulation, Bax and Bak activation, and Mcl-1 elimination.

Journal: Molecular pharmacology 20050601

Title: Phase I study of the farnesyltransferase inhibitor BMS-214662 given weekly in patients with solid tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20050601

Title: Isoprenylation of intracellular proteins as a new target for the therapy of human neoplasms: preclinical and clinical implications.

Journal: Current drug targets 20050501

Title: Phase I study of BMS-214662, a farnesyl transferase inhibitor in patients with acute leukemias and high-risk myelodysplastic syndromes.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20050420

Title: Phase I pharmacokinetic and pharmacodynamic study of weekly 1-hour and 24-hour infusion BMS-214662, a farnesyltransferase inhibitor, in patients with advanced solid tumors.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20050410

Title: A phase I trial of the novel farnesyl protein transferase inhibitor, BMS-214662, in combination with paclitaxel and carboplatin in patients with advanced cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20050301

Title: [Farnesyltransferase inhibitors: preliminary results in acute myeloid leukemia].

Journal: Bulletin du cancer 20050301

Title: Clinical activity of farnesyl transferase inhibitors in hematologic malignancies: possible mechanisms of action.

Journal: Leukemia & lymphoma 20041101

Title: Farnesyltransferase inhibitor BMS-214662 induces apoptosis in B-cell chronic lymphocytic leukemia cells.

Journal: Leukemia 20041001

Title: Crystal structures of the anticancer clinical candidates R115777 (Tipifarnib) and BMS-214662 complexed with protein farnesyltransferase suggest a mechanism of FTI selectivity.

Journal: Biochemistry 20040608

Title: Apoptotic and cytostatic farnesyltransferase inhibitors have distinct pharmacology and efficacy profiles in tumor models.

Journal: Cancer research 20040601

Title: A phase I pharmacokinetic and pharmacodynamic study of the farnesyl transferase inhibitor BMS-214662 in combination with cisplatin in patients with advanced solid tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20040415

Title: Phase I clinical trial of the farnesyltransferase inhibitor BMS-214662 given as a 1-hour intravenous infusion in patients with advanced solid tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20040401

Title: Synthesis of N,N'-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20040209

Title: Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.

Journal: Journal of medicinal chemistry 20040129

Title: Farnesyl transferase inhibitors in myeloid malignancies.

Journal: Blood reviews 20030901

Title: Farnesyltransferase inhibitors in acute myeloid leukemia and myelodysplastic syndromes.

Journal: Clinical lymphoma 20030801

Title: Preclinical and clinical evaluation of farnesyltransferase inhibitors.

Journal: Current oncology reports 20030301

Title: Farnesyl transferase inhibitors in the treatment of breast cancer.

Journal: Expert opinion on investigational drugs 20030301

Title: Targeting RAS signalling pathways in cancer therapy.

Journal: Nature reviews. Cancer 20030101

Title: BMS-214662 (Bristol-Myers Squibb).

Journal: IDrugs : the investigational drugs journal 20030101

Title: Farnesyl transferase inhibitors as anticancer agents.

Journal: European journal of cancer (Oxford, England : 1990) 20020901

Title: [New therapeutic targets and strategies in lung cancer].

Journal: Archivos de bronconeumologia 20020801

Title: Agents targeting ras signaling pathway.

Journal: Current pharmaceutical design 20020101

Title: Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor.

Journal: Cancer research 20011015

Title: Farnesyltransferase inhibitors.

Journal: Seminars in oncology 20011001

Title: 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.

Journal: Journal of medicinal chemistry 20001005

Title: Hunt JT, et al. 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. J Med Chem. 2000 Oct 5;43(20):3587-95.

Title: Rose WC, et al. Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor. Cancer Res. 2001 Oct 15;61(20):7507-17.

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