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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
BMS-214662
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
195987-41-8
- 规格：
10mg/1mg/5mg
| 规格： | 10mg | 产品价格： | ￥4790.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥1580.0 |
| 规格： | 5mg | 产品价格： | ￥3190.0 |
| 基本信息 | |
| CAS | No.195987-41-8 |
| 英文名称 | BMS-214662 |
| 别名 | ;Imidalinehydrochloride;NSC35110hydrochloride; |
| 分子式 | C25H23N5O2S2 |
| 分子量 | 489.61 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES | C1C(N(CC2=C(N1CC3=CN=CN3)C=CC(=C2)C#N)S(=O)(=O)C4=CC=CS4)CC5=CC=CC=C5 |
| InChIKey | OLCWFLWEHWLBTO-HSZRJFAPSA-N |
| InChI | 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 |
| PubChem CID | 448545 |
| 靶点 | Farnesyl Transferase |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | BMS-214662是有效选择性的farnesyl transferase抑制剂，具有抗肿瘤活性。 |
| 生物活性 | BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM.[1-2] |
| IC50 | IC50: 1.35 nM (farnesyl transferase)， 1.3 μM (Ras-CVLL)， 2.3 μM (K-Ras)[1] |
| 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]. |
| 细胞实验 | 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]. |
| 细胞实验 | 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]. |
| 动物实验 | 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]. |
| 数据来源文献 | [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. 200 [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. |
| 单位 | 瓶 |
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