(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile

(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile Suppliers list
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Products Intro: Product Name:(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile
CAS:195987-41-8
Purity:99% Package:100g ;1KG ;5KG 25KG
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Products Intro: Product Name:7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine
CAS:195987-41-8
Purity:97+% Package:1g;10g;100g;;1kg Remarks:Z-27209
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Products Intro: Product Name:BMS-214662
CAS:195987-41-8
Purity:98.00% Package:1 mL * 10mM (in DMSO);10 mg;100 mg;200 mg;25 mg;5 mg;50 mg;500 mg Remarks:REAGENT;FOR LABORATORY USE ONLY
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Products Intro: Product Name:BMS-214662
CAS:195987-41-8
Purity:98% Package:5mg Remarks:V3486
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Products Intro: Product Name:1H-1,4-Benzodiazepine-7-carbonitrile,2,3,4,5-tetrahydro-1-(1H-iMidazol-5-ylMethyl)-3-(phenylMethyl)-4-(2-thienylsulfonyl)-,(3R)-
CAS:195987-41-8
Purity:0 Package:1g; 5g; 25g; 1kg; 5kg; 25kg Remarks:0
(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile Basic information
Product Name:(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile
Synonyms:(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile;1H-1,4-Benzodiazepine-7-carbonitrile,2,3,4,5-tetrahydro-1-(1H-iMidazol-5-ylMethyl)-3-(phenylMethyl)-4-(2-thienylsulfonyl)-,(3R)-;(3R)-2,3,4,5-Tetrahydro-1-(1H-iMidazol-4-ylMethyl)-3-(phenylMethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-carbonitrile;(R)-2,3,4,5-Tetrahydro-1-(1H-iMidazol-4-ylMethyl)-3-(phenylMethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-ca;BMS214662; BMS 214662;7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine;(3R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-5-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-carbonitrile
CAS:195987-41-8
MF:C25H23N5O2S2
MW:489.61
EINECS:
Product Categories:Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds
Mol File:195987-41-8.mol
(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile Structure
(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile Chemical Properties
Boiling point 790.9±70.0 °C(Predicted)
density 1.45±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO: slightly soluble; Methanol: slightly soluble
form A solid
pka13.19±0.10(Predicted)
Safety Information
MSDS Information
(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile Usage And Synthesis
DescriptionBMS 214662 is a potent inhibitor of farnesyltransferase (FTase; IC50 = 1.3 nM). It is selective for FTase over geranylgeranyl transferase (GGTase; IC50 = 1,900 nM). It inhibits the growth of MEK2, A2780, and PC3 cancer cells expressing wild-type Ras (IC50s = 2.5, 0.04, and 0.15 μM, respectively), as well as HCT116, MIP, RC-165, and MIA PaCa-2 cells expressing mutant K-Ras (IC50s = 0.06, 0.3, 0.3, and 0.12 μM, respectively). BMS 214662 induces apoptosis in HCT116 cells in a concentration-dependent manner. In vivo, BMS 214662 (600 mg/kg) is curative in an HCT116 mouse xenograft model. It also reduces tumor growth in Calu-1, HT-29, EJ-1, and MIA PaCa-2 mouse xenograft models.
Chemical PropertiesPale Yellow Solid
UsesA potent and selective inhibitor of farnesyltransferase that induces mitochondrial apoptosis in chronic myeloid leukemia stem/progenitor cells, including CD34+38- cells, through activation of protein kinase Cβ.
DefinitionChEBI: BMS-214662 is a member of the class of benzodiazepines that is 2,3,4,5-tetrahydro-1H-1,4-benzodiazepine substituted by (1H-imidazol-5-yl)methyl, benzyl, (thiophen-2-yl)sulfonyl, and cyano groups at positions 1, 3R, 4 and 7, respectively. It is a potent inhibitor of farnesyltransferase (IC50 = 1.35nM) which was under clinical development for the treatment of solid tumors. It has a role as an antineoplastic agent, an apoptosis inducer and an EC 2.5.1.58 (protein farnesyltransferase) inhibitor. It is a member of imidazoles, a nitrile, a member of thiophenes, a sulfonamide, a member of benzenes and a benzodiazepine.
(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile Preparation Products And Raw materials
Tag:(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile(195987-41-8) Related Product Information