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当前位置: 首页 > 信号通路研究 > PI3K > CH5132799
CH5132799
CH5132799
CH5132799
商品货号:MB3434
CAS 号:1007207-67-1
英文名字:CH5132799
质量标准:>98%, I型 PI3Ks抑制剂
分子式:C15H19N7O3S
  • 包装规格:
    规格 库存 发货时间
    5MG [¥980.00]15 现货
    10MG [¥1600.00]15 现货
    50MG [¥5800.00]15 现货
  • 购买数量:
  • 会员尊享价:

    商品信息

    质检证书(coa)

    说明书下载

     CH-5132799

    分子式:C15H19N7O3S  分子量:377.42

     

    产品描述

    CH5132799抑制 I PI3Ks, 尤其是PI3KαIC5014 nM; PI3Kβδγ作用效果稍弱PIK3CA突变型细胞系敏感。

    靶点

    PI3Kα

    PI3Kβ

    PI3Kδ

    PI3Kγ

       

    IC50

    0.014 μM

    0.12 μM

    0.50 μM

    0.036 μM

       

    体外研究

    CH5132799 selectively inhibits class I PI3Ks, PI3Kα (IC50 = 0.014 μM ), PI3Kβ (IC50 = 0.12 μM ), PI3Kδ (IC50 = 0.50 μM ), PI3Kγ (IC50 = 0.036 μM ), but shows less inhibition of class II PI3Ks, class III PI3k and mTOR and also no inhibitory activity (IC50 > 10 μM) against 26 protein kinases. CH5132799 exhibits more inhibitory activities against PI3Kα with oncogenic mutations E542K (IC50 = 6.7 nM), E545K (IC50 = 6.7 nM) and H1047R (IC50 = 5.6 nM) than wild-type PI3Kα. CH5132799 treated breast cnacer KPL-4 cells, which harbor the PIK3CA mutation, phosphorylation of Akt and its direct substrates, PRAS40 and FoxO1/3a and phosphorylation of downstream factors, including S6K, S6 and 4E-BP1, are effectively suppressed. Cancer cell lines harboring PIK3CA mutations are significantly sensitive to CH5132799 In human tumor cell lines with PI3K pathway activation by mutation, CH5132799 shows potent antiproliferative activity [HCT116(CRC): IC50 = 0.20 lM, KPL-4(BC):13 IC50 = 0.032 lM, T-47D(BC): IC50 = 0.056 lM, SK-OV-3(Ovarian): IC50 = 0.12 lM]. CH5132799 effectively suppresses phosphorylation of AKT in KPL-4 cells.

    体内研究

    CH5132799 shows potent in vivo antitumor activity in several different xenograft models with PIK3CA mutations. CH5132799 overcomes mTORC1 inhibition-mediated Akt activation and regrowth of xenograft tumor by long-term everolimus administration.CH5132799 as a clinical candidate that shows excellent oral bioavailability (BA) (101% in mouse), human liver microsomal stability and in vivo antitumor activity in the PC-3 xenograft model (TGI: 101% at 25 mg/kg, po, q.d. × 11 days). CH5132799 exhibits good oral BA in mouse, rat, monkey and dog (F: 54.2-101%). In a human breast cancer (KPL-4: PI3Ka H1047R) xenograft model in mice, oral treatment with CH5132799 (12.5 mg/kg, q.d.) shows strong tumor regression. The strong regression is maintained during the 6 week administration, even in the intermittent dosing schedule (q.d., 2 weeks on/1 week off; q.d., 5 days on/2 days off), suggesting that a flexible administration schedule can be applicable in the clinic.

    溶解性

    DMSO 12 mg/mL,水 <1 mg/mL,乙醇 <1 mg/mL

    稳定性

    2 -20°C粉状,6-80°C溶于DMSO

    特征

           

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    http://www.meilune.com/article.php?id=374

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