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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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文献和实验bSuKm1foWOq5wNpboNQLmlo2Fn6wS/ZjqQvb2Gy88CULhuQ5TVEaoQ2gtdU9TtPRtFgh/BbLYDrlNQtO4GHJJVoXvFg0UhwMJHFBz8InEEZPh1ZysOf82LTuunw2ReE8zcuwcvBs9FhSwx9ygL9MIXF3cE5dCHQW6tUCFBRmfdHz/iB3LBwEAHsR9N0y8571/wU9NGdk3x4RpaZL/f4OLeO2i7bi76ls+Z7gQPsYry5csjR44c9GX7BuIIRl9f
释放，任何由 DW12 品系衍生出的品系可以用作牲畜词料……”。同样，“自 2006 年 6 月 22 日起，普通小麦品系 BW255-2 和 BW238-3 也被批准环境释放和用作牲畜伺料”。尽管上述品系已通过审批，但能否完全商业化还不能确定。 4.2 耐虫性 最近与耐虫性相关的研究报道有：利用豇豆胰蛋白酶抑制剂防治麦蛾（Sitotroga cerealella Olivier) [ 22 ] , 利用马铃暮蛋白酶抑制剂（PIN2 ) 防治线虫 [23]。 4.3 耐病性
1. 介绍 包含非天然氨基酸的蛋白质的过量表达已引起越来越多科学家的关注。作为一个例子，非天然氨基酸的定点掺入，使关于蛋白质结构和功能的化学假定的特异检测成为可能。类似地，具有新化学性质的非天然氨基酸的定点掺入，可能使蛋白质产生新的功能，如与酮基取代的氨基酸交联 [1] 。对整个蛋白质的整体非天然氨基酸掺入，也可能导 致新的物理或功能性质。例如，用硒代甲硫氨酸那样的重原子类似物代替甲硫氨酸，已成为 X 射线晶体学中得到差值图（进而得到位相，解析蛋白质晶体结构——译者注）的有用
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