基本属性 生物活性体外研究体内研究特征 用途与合成方法 供应商 相关产品
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2-[(2-氯-4-碘苯基)氨基]-N-(环丙基甲氧基)-3,4-二氟-苯甲酰胺

基本属性 生物活性体外研究体内研究特征 用途与合成方法 供应商 相关产品
2-[(2-氯-4-碘苯基)氨基]-N-(环丙基甲氧基)-3,4-二氟-苯甲酰胺
2-[(2-氯-4-碘苯基)氨基]-N-(环丙基甲氧基)-3,4-二氟-苯甲酰胺 性质
  • 熔点 166-169°C
  • 储存条件 -20°C Freezer
  • 溶解度 DMSO: ≥30mg/mL
  • 颜色white to tan
2-[(2-氯-4-碘苯基)氨基]-N-(环丙基甲氧基)-3,4-二氟-苯甲酰胺 用途与合成方法
  • 生物活性PD184352 (CI-1040)是一种ATP非竞争性的MEK1/2抑制剂,IC50为17 nM,对MEK1/2的选择性比MEK5高100倍。Phase 2。
  • 体外研究CI-1040 treatment produces a reduction of pMAPK levels in multiple tumor cells including Colon 26, BX-PC3 pancreatic, A431 cervical, HT-29 colon, ZR-25-1 breast and SKOV-3 ovarian carcinomas. CI-1040 treatment doesn't inhibit the phosphorylation of Jun kinase, p38 kinase or Akt, indicating CI-1040 specifically targets MEK. Inhibition of MAPK activation by CI-1040 prevents cell cycle progression and induces a G1 block. The IC50 for inhibition of MEK1 by CI-1040 is 0.3 μM, 15-fold higher than the concentration required to inhibit the EGF-induced activation of ERK2 in Swiss 3T3 cells. These results indicate CI-1040 exerts its effects on cells by suppressing the activation of MKK1, and not by blocking its activity. 2 nM PD184352 inhibits the activation of MKK1 in Swiss 3T3 cells by 50%, while over 100-fold concentration of CI-1040 inhibits MEK1 in vitro. PD184352 also inhibits the Raf-catalysed phosphorylation of MEK1 without any effect on the Raf-catalysed phosphorylation of myelin basic protein. CI-1040 inhibits 86% of papillary thyroid carcinoma (PTC) cell growth with the RET/PTC1 rearrangement at 10μM compared with cells treated with DMSO only. CI-1040 shows potent inhibition to PTC cells (BRAF mutation) with GI50 of 52 nM, but low activity to RET/PTC1 rearrangement type with GI50 of 1.1 μM. A recent research indicates CI-1040 increases the apoptotic effect of BMS-214662 in a CML blast crisis cell line, K562, and in primary chronic phase CD34+ CML cells.
  • 体内研究Oral dosing of CI-1040 impairs the growth of colon tumor xenografts of mouse and human with a wide dose range of 48-200 mg/kg per dose, but not of P388 leukemia. CI-1040 inhibits the tumor xenografts from PTC cells carrying a BRAF mutation with 31.3% reduction, carrying the RET/PTC1 rearrangement with 47.5% reduction than in untreated (vehicle) mice after 3 weeks of oral administration (300 mg/kg/d). No toxic effects are observed in any mice when they are treated with CI-1040. Transient exposure of mammary tumors to CI-1040 and UCN-01 causes tumor cell death in vivo and prolonged suppression of tumor regrowth. Combined treatment with CI-1040 (25 mg/kg) and UCN-01 (0.1-0.2 mg/kg) significantly reduces MDA-MB-231, and largely abolishs MCF7 tumor growth in implanted athymic mice, while either single treatment has no significant activity. The drug combination leads to profound tumor cell death which correlates with a reduction in the phosphorylation of ERK1/2 and the immuno-reactivity of Ki67 and of CD31.
  • 特征First MEK inhibitor to begin clinical development.
安全信息
  • 危险品标志 N
  • 危险类别码 50/53
  • 安全说明 60-61
  • 危险品运输编号 UN 3077 9 / PGIII
2-[(2-氯-4-碘苯基)氨基]-N-(环丙基甲氧基)-3,4-二氟-苯甲酰胺供应商更多
  • 公司名称:上海波以尔化工有限公司
  • 联系电话:86-15221043597
  • 产品介绍: 中文名称:2-[(2-氯-4-碘苯基)氨基]-N-(环丙基甲氧基)-3,4-二氟-苯甲酰胺
    英文名称:CI 1040
    CAS:212631-79-3
    纯度:95%min
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  • 公司名称:百灵威科技有限公司
  • 联系电话:400-666-7788 +86-10-82848833
  • 产品介绍: 中文名称:2-[(2-氯-4-碘苯基)胺]-N-(环丙基甲氧基)-3,4-二氟苯甲胺
    英文名称:PD-184352
    CAS:212631-79-3
    包装信息:100Mg,10Mg,25Mg 备注:化学试剂、精细化学品、医药中间体、材料中间体
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  • 公司名称:上海佰世凯化学科技有限公司
  • 联系电话:+86(0)21-20908456
  • 产品介绍: 英文名称:PD 184352(CI-1040)
    CAS:212631-79-3
    备注:C13991
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  • 公司名称:凯方医药科技(上海)有限公司
  • 联系电话:021-67220633 & 021-37212706
  • 产品介绍: 英文名称:2-(2-Chloro-4-iodophenylaMino)-N-(cyclopropylMethoxy)-3,4-difluorobenzaMide
    CAS:212631-79-3
    纯度:99% 包装信息:5KG;1KG
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  • 公司名称:凯试(上海)科技有限公司
  • 联系电话:021-50135380
  • 产品介绍: 英文��称:PD-184352
    CAS:212631-79-3
    纯度:98% 备注:1500元/10mg; 3229元/25mg; 6500元/100mg
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