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- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
LNK-754; OSI-754
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2091.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥850.0 |
| 规格： | 5 mg | 产品价格： | ￥1980.0 |
| 规格： | 10 mg | 产品价格： | ￥3200.0 |
| 规格： | 25 mg | 产品价格： | ￥5450.0 |
| 规格： | 50 mg | 产品价格： | ￥7500.0 |
| 规格： | 100 mg | 产品价格： | ￥9800.0 |
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CP-609754
CAS No. : 1190094-64-4
MCE 国际站：CP-609754
产品活性：CP-609754 (LNK-754) 是一种有效且可逆的法尼基转移酶(farnesyltransferase) 抑制剂，具有潜在的抗癌活性。CP-609754 抑制重组人 H-Ras 和重组 K-Ras法尼基化的 IC50 分别为 0.57 ng/mL 和 46 ng/mL。CP-609754 是一种点击化学试剂。它含有 Alkyne 基团，可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。
研究领域：Metabolic Enzyme/Protease
作用靶点：Farnesyl Transferase
In Vitro: CP-609754 (CP-609,754) is a reversible inhibitor of farnesyltransferase with a slow on/off rate. CP-609,754 inhibits farnesylation (IC50=1.72 ng/mL) of mutant H-Ras in 3T3 H-ras (61L)-transfected cell lines with SDS-PAGE analysis of [35S]methionine-labeled material.
?CP-609754 is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI. CP-609754 interacts with the farnesyltransferase-farnesyl PPI complex and competes for the binding of the Ras protein. CP-609754 selectively inhibits farnesylation of both H- and K-Ras proteins in 3T3 transfectants.
In Vivo: CP-609754 (CP-609,754) has antitumor activity against 3T3 H-ras (61L) tumors in vivo.
?With twice daily oral dosing of CP-609754, tumor regression is achieved with a dose of 100 mg/kg; the ED50 for tumor growth inhibition is 28 mg/kg.?
?With continuous i.p. infusion of CP-609754, tumor growth is inhibited by >50%, and tumor farnesyltransferase activity inhibited by >30% in mice in which the plasma concentration of CP-609754 is maintained above 118 ng/mL.
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Isolation of CP43 and CP47 Photosystem II Proximal Antenna Complexes From Plants
A single-column method to purify the CP43 and CP47 pigment-protein complexes of photosystem (PS)II from higher plants is presented. To validate the isolation procedure, three different species were used (Spinacea oleracea, Beta vulgaris
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