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Pictilisib

RG7321,GDC-0941

GDC-0941是一种有效的PI3Kα/δ抑制剂，IC50为3 nM，比对p110β(10倍)和p110γ的作用强25倍。

目录号
EY1082
EY1082
EY1082
纯度
99.25%
99.25%
99.25%
规格
1 mg
5 mg
10 mg
原价
200
500
750
售价
200
500
750
库存
现货
现货
现货
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  • 生物活性

    GDC-0941 is a potent small-molecule thieno [3, 2-d] pyrimidine inhibitor of the class I PI3K. It is highly selective against isoforms p110( and p110( with IC50 of 3 nM, and moderately selective against isoforms p110( and p110( with IC50s of 33 nM and 75 nM, respectively.GDC-0941 inhibits cell proliferation in vitro and in vivo. It causes growth inhibition in a variety of cancer cell lines, including A2780, MDA-MB-361, PC3, and U87MG. It also inhibits the growth of trastuzumab–sensitive and –resistant HER2-amplied cancer cells which harbor p110( mutations or PTEN loss. GDC-0941 also reduces tumor volume in different xenograft models.

  • 体外研究

  • 体内研究

    1% DMSO+30% polyethylene glycol+1% Tween 80

  • 激酶实验

  • 细胞实验

    ~10 μM

  • 动物实验

    ~150 mg/kg/day 口服饲喂

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Folkes AJ, et al. J Med Chem, 2008, 51(18), 5522-5532.
    [2] Wallin JJ, Guan J, Prior WW, Lee LB, Berry L, Belmont LD, Koeppen H, Belvin M, Friedman LS, Sampath D.GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of docetaxel in human breast cancer models by increasing cell death in vitro and in vivo.Clin Cancer Res. 2012 Jul 15;18(14):3901-11. Epub 2012 May 14.
    [3] Zou ZQ, Zhang LN, Wang F, Bellenger J, Shen YZ, Zhang XH.The novel dual PI3K/mTOR inhibitor GDC-0941 synergizes with the MEK inhibitor U0126 in non-small cell lung cancer cells.Mol Med Report. 2012 Feb;5(2):503-8.

    分子式
    C23H27N7O3S2    		 分子量
    513.64    		 CAS号
    957054-30-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    45 mg/ml     		Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00996892 Solid Tumors Drug: Cobimetinib|Drug: Pictilisib Genentech, Inc. Phase 1 2009-11-01 2016-11-04
    NCT00960960 Breast Cancer Drug: Bevacizumab|Drug: Pictilisib|Drug: Letrozole|Drug: Paclitaxel|Drug: Trastuzumab Genentech, Inc. Phase 1 2009-08-01 2016-12-14
    NCT00876109 Solid Cancers Drug: GDC-0941 Genentech, Inc. Phase 1 2007-10-01 2016-11-01
    NCT02092831 Healthy Volunteer Drug: GDC-0941|Drug: GDC-0941|Drug: GDC-0941|Drug: GDC-0941 Genentech, Inc. Phase 1 2014-04-01 2016-11-01
    NCT02389842 Advanced Solid Tumours|Breast Cancer Drug: Palbociclib + Taselisib / Pictilisib Royal Marsden NHS Foundation Trust|Institute of Cancer Research, United Kingdom|Roche Pharma AG|Pfizer Phase 1 2015-02-01 2015-03-16
    NCT01918306 Estrogen Receptor Negative Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Triple Negative Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer|Triple-negative Breast Cancer Drug: cisplatin|Other: laboratory biomarker analysis|Other: pharmacological study|Procedure: dynamic contrast-enhanced MRI, diffusion-weighted MRI & chemical exchange saturation transfer MRI|Drug: GDC -0941 Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI)|Genentech, Inc. Phase 1|Phase 2 2013-09-01 2015-08-17
    NCT00876122 Non-Hodgkin's Lymphoma, Solid Cancers Drug: GDC-0941 Genentech, Inc. Phase 1 2008-03-01 2016-11-01
    NCT01740336 Breast Cancer Drug: GDC-0941|Drug: Placebo|Drug: paclitaxel Genentech, Inc. Phase 2 2013-02-01 2015-05-28
    NCT00975182 Non-Squamous Non-Small Cell Lung Cancer, Solid Cancers Drug: GDC-0941|Drug: erlotinib HCl Genentech, Inc. Phase 1 2009-09-01 2016-11-01
    NCT01474668 Healthy Volunteer Drug: GDC-0941 Genentech, Inc. Phase 1 2011-10-01 2016-11-01
    NCT01240226 Healthy Volunteer Drug: GDC-0941|Drug: GDC-0941|Drug: ketoconazole Genentech, Inc. Phase 1 2010-11-01 2017-03-02
    NCT00999128 Healthy Volunteers Drug: GDC-0941|Drug: rabeprazole Genentech, Inc. Phase 1 2009-10-26 2017-02-07
    NCT01437566 Breast Cancer Drug: Fulvestrant|Drug: GDC-0941|Drug: GDC-0941 Matching Placebo|Drug: GDC-0980|Drug: GDC-0980 Matching Placebo Genentech, Inc. Phase 2 2011-10-01 2016-11-01
    NCT00928330 Metastatic Breast Cancer Drug: GDC-0941|Drug: Trastuzumab|Drug: trastuzumab-MCC-DM1 Genentech, Inc. Phase 1 2009-07-01 2016-11-01
    NCT00974584 Non-Squamous Non-Small Cell Lung Cancer Drug: GDC-0941|Drug: bevacizumab|Drug: carboplatin|Drug: cisplatin|Drug: paclitaxel|Drug: pemetrexed Genentech, Inc. Phase 1 2009-10-01 2016-11-01
    NCT01493843 Non-Squamous Non-Small Cell Lung Cancer Drug: GDC-0941|Drug: Placebo|Drug: bevacizumab|Drug: carboplatin|Drug: paclitaxel Genentech, Inc. Phase 2 2012-01-01 2016-11-01
    NCT02430363 Glioblastoma Drug: MK - 3475|Biological: Suppressor of the PI3K/Akt pathways Medical Research Council|Department of Experimental Clinical Oncology, Aarhus University Hospital|NCRI Clinical Studies Groups|ECCO - the European CanCer Organisation|Merck Sharp & Dohme Corp. Phase 1|Phase 2 2013-03-01 2016-02-23

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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