Introduction：Basic information about CAS 195987-41-8|BMS 214662, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | BMS 214662 |
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| CAS Number | 195987-41-8 | Molecular Weight | 489.61200 |
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| Density | 1.45g/cm3 | Boiling Point | 790.9ºC at 760mmHg |
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| Molecular Formula | C25H23N5O2S2 | Melting Point | / |
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| MSDS | / | Flash Point | 432.1ºC |
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Names
| Name | (3R)-3-benzyl-1-(1H-imidazol-5-ylmethyl)-4-thiophen-2-ylsulfonyl-3,5-dihydro-2H-1,4-benzodiazepine-7-carbonitrile |
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| Synonym | More Synonyms |
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BMS 214662 BiologicalActivity
| Description | BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM. |
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| Related Catalog | Signaling Pathways >>Metabolic Enzyme/Protease >>Farnesyl TransferaseResearch Areas >>Cancer |
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| Target | IC50: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)[1] |
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| In Vitro | BMS-214662 is over 1000-fold selective for farnesyl transferase, having IC50 values for inhibition of geranylgeranylation of Ras-CVLL and K-Ras of 1.3 and 2.3 μM, respectively[1]. BMS-214662 shows good potency in inhibiting H-ras-transformed rodent cells, A2780 human ovarian carcinoma tumor cells, and HCT-116 human colon carcinoma tumor cells. BMS-214662 is the most potent apoptotic FTI known and demonstrates broad spectrum yet robust cell-selective cytotoxic activity against a panel of cell lines with diverse histology[2]. |
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| In Vivo | Tumors from BMS-214662-treated mice have increased numbers of apoptotic cells as compared with the nontreated control mice. The AIs in HCT-116 tumors are increased 4-10-fold in BMS-214662-treated mice as compared with nontreated controls. BMS-214662 is significantly cytotoxic to both HCT-116 and EJ-1 tumor cells; the doses of BMS-214662 required to kill 90% of clonogenic tumor cells are approximately 75 and 100 mg/kg for HCT-116 and EJ-1 tumors[2]. |
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| Cell Assay | The hydrochloride salt of BMS-214662 is dissolved in DMSO with dilutions made using either water or RPMI 1640 plus 10% fetal bovine serum. BMS-214662 is added at various concentrations. The cells are incubated at 37°C for 72 h, at which time MTS in combination with phenazine methosulfate is added. After an additional 3 h, the absorbance is measured at 492 nm, and the growth inhibition results are eventually expressed as IC50s[2]. |
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| Animal Admin | Mice: BMS-214662 is dissolved in ethanol, followed by dilution with water to a final ethanol concentration of 10%. Mice implanted with HCT-116 xenografts are administered a single dose of BMS-214662 at 250 mg/kg i.v., 300 mg/kg i.p., or 400 mg/kg p.o. An additional group receives 400 mg/kg BMS-214662 daily for 2 days (administered p.o. on day 1 and i.p. on day 2). Nontreated mice with time-matched HCT-116 tumors served as controls. Tumors are collected at 24 h after dose, processed following standard methods, sectioned, and stained with H&E. Serial sections of each tumor are processed for in situ apoptotic cell labeling by the TUNEL method[2]. |
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| References | [1]. 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. [2]. 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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Chemical & Physical Properties
| Density | 1.45g/cm3 |
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| Boiling Point | 790.9ºC at 760mmHg |
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| Molecular Formula | C25H23N5O2S2 |
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| Molecular Weight | 489.61200 |
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| Flash Point | 432.1ºC |
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| Exact Mass | 489.12900 |
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| PSA | 129.71000 |
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| LogP | 5.24898 |
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| Vapour Pressure | 5.38E-25mmHg at 25°C |
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| Index of Refraction | 1.722 |
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| InChIKey | OLCWFLWEHWLBTO-HSZRJFAPSA-N |
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| SMILES | N#Cc1ccc2c(c1)CN(S(=O)(=O)c1cccs1)C(Cc1ccccc1)CN2Cc1cnc[nH]1 |
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| Storage condition | 2-8℃ |
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Synonyms
| 3-BENZYL-1-(1H-IMIDAZOL-4-YLMETHYL)-4-(THIEN-2-YLSULFONYL)-2,3,4,5-TETRAHYDRO-1H-1,4-BENZODIAZEPINE-7-CARBONITRILE |
| BMV |
| (R)-1-((1H-imidazol-5-yl)methyl)-3-benzyl-4-(thiophen-2-ylsulfonyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile |
| BMS-214662 |
