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当前位置: 首页 > 信号通路研究 > MEK > PD184352 (CI-1040)
PD184352 (CI-1040)
PD184352 (CI-1040)
PD184352 (CI-1040)
商品货号:MB5452
CAS 号:212631-79-3
英文名字:PD-184352 (CI-1040)
质量标准:>99%,MEK1/2抑制剂
分子式:C17H14ClF2IN2O2
  • 包装规格:
    规格 库存 发货时间
    25MG [¥300.00]15 现货
    100MG [¥800.00]15 现货
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    商品信息

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     PD184352 (CI-1040)

    分子式:C17H14ClF2IN2O2    分子量:478.66
     
     

    产品描述

    CI-1040 (PD 184352)ATP非竞争性的MEK1/2抑制剂,IC5017 nM, 作用于MEK1/2 比作用于MEK5选择性高100倍。

    靶点

    MEK1

    MEK2

           

    IC50

    17 nM

    17 nM

           

    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.

    溶解性

    DMSO 96 mg/mL,水 <1 mg/mL,乙醇 14 mg/mL

    稳定性

    2 -20°C粉状,6-80°C溶于DMSO

    特征

    First MEK inhibitor to begin clinical development.

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