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OSI-906

Linsitinib

Linsitinib(OSI-906)是口服活性的ATP竞争性IGF-1R和insulin受体双重抑制剂，IC50分别为35 nM和75 nM。

目录号
EY1647
EY1647
EY1647
EY1647
EY1647
纯度
99.23%
99.23%
99.23%
99.23%
99.23%
规格
2 mg
5 mg
10 mg
50 mg
100 mg
原价
680
990
1760
4600
7900
售价
680
990
1760
4600
7900
库存
现货
现货
现货
现货
现货
订购
订购
订购
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  • 生物活性

    OSI-906 (Linsitinib) is an orally bioavailable, potent small molecular dual inhibitor of IGF-1R and InsR with IC50 of 35 nM and 75 nM. OSI-906 through its inhibition of both IGF-1R and IR, prevents ligand-induced activation of downstream pathways including pAKT, pERK1/2 and p-p70S6K and, therefore, inhibits proliferation in a variety of tumor cell lines. OSI-906 displayed robust in vivo anti-tumor efficacy in an IGF-1R-driven xenograft model when administered orally.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% propylene glycol

  • 激酶实验

  • 细胞实验

    0.02-0.8 μM

  • 动物实验

    25 mg/kg和75 mg/kg 口服处理，每天一次，持续14天

  • 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] Mulvihill MJ, et al. Future Med Chem, 2009, 1(6), 1153-1171.

    分子式
    C26H23N5O    		 分子量
    421.49    		 CAS号
    867160-71-2    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    80 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
    NCT01529684 Advanced Solid Tumors|Pharmacokinetics of 14C-OSI-906 Drug: radio-labeled OSI-906|Drug: OSI-906 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Phase 1 2012-01-01 2013-04-12
    NCT01016860 Colorectal Cancer Drug: OSI-906|Drug: irinotecan University of Colorado, Denver Phase 1 2009-12-01 2013-10-18
    NCT00514306 Advanced Solid Tumors Drug: OSI-906 Astellas Pharma Inc Phase 1 2007-06-01 2011-09-12
    NCT00924989 Adrenocortical Carcinoma Drug: OSI-906|Other: Placebo Astellas Pharma Inc Phase 3 2009-09-01 2013-07-10
    NCT00514007 Advanced Solid Tumors Drug: OSI-906 Astellas Pharma Inc Phase 1 2006-12-01 2012-04-16
    NCT01221077 Non Small Cell Lung Cancer|NSCLC Drug: OSI-906|Drug: Erlotinib|Drug: Placebo Astellas Pharma Inc Phase 2 2011-12-01 2014-10-03
    NCT01334710 Liver Cancer Drug: Sorafenib and OSI-906 Emory University|OSI Pharmaceuticals Phase 2 2011-03-01 2013-11-18
    NCT01101906 Advanced Hepatocellular Carcinoma (HCC) Drug: OSI-906|Drug: Placebo Astellas Pharma Inc Phase 2 2010-10-01 2012-12-10
    NCT01600807 Pancreatic Cancer, Metastatic Drug: Gemcitabine, Erlotinib, OSI-906|Drug: Gemcitabine, Erlotinib Dana-Farber Cancer Institute Phase 1|Phase 2 null 2013-06-25
    NCT00739453 Advanced Solid Tumors Drug: OSI-906|Drug: erlotinib Astellas Pharma Inc Phase 1 2008-10-01 2011-12-21
    NCT01205685 Hormone-sensitive Metastatic Breast Cancer Drug: OSI-906|Drug: Erlotinib|Drug: Letrozole|Drug: Goserelin Vanderbilt-Ingram Cancer Center Phase 2 2010-05-01 2012-08-10
    NCT01186861 Non-Small Cell Lung Cancer (NSCLC) With Nonprogression Following 4 Cycles of Platinum-based Chemotherapy Drug: OSI-906|Drug: erlotinib|Drug: placebo Astellas Pharma Inc Phase 2 2010-12-01 2015-04-07
    NCT01154335 Metastatic Colorectal Cancer Drug: OSI-906|Drug: Everolimus SCRI Development Innovations, LLC|Novartis Pharmaceuticals|OSI Pharmaceuticals Phase 1 2010-07-01 2015-01-06
    NCT00889382 Solid Tumors|Ovarian Cancer Drug: OSI-906|Drug: Paclitaxel Astellas Pharma Inc Phase 1|Phase 2 2009-07-01 2014-09-22
    NCT01533246 Adenocarcinoma of the Prostate|Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer Drug: linsitinib|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2012-02-01 2015-03-02
    NCT01567384 Cancer|Neoplasms|Tumors Drug: OSI-906 and Pemetrexed Emory University|OSI Pharmaceuticals Phase 1 2012-05-01 2013-11-19
    NCT01427205 Head and Neck Cancer Drug: Cetuximab|Drug: OSI-906|Other: Placebo M.D. Anderson Cancer Center|OSI Pharmaceuticals Phase 2 2013-06-01 2013-04-04
    NCT01013506 Breast Cancer Drug: IGF-1R inhibitor OSI-906|Drug: erlotinib hydrochloride|Drug: goserelin|Drug: letrozole Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) Phase 2 2009-08-01 2013-05-22
    NCT02546544 Relapsed Ewing Sarcoma|Refractory Ewing Sarcoma Drug: Linsitinib University of Oxford|European Organisation for Research and Treatment of Cancer - EORTC|European Commission|Astellas Pharma Inc|Oxford University Hospitals NHS Trust Phase 2 2014-03-01 2017-03-21
    NCT01560260 Carney Complex|Chondrosarcoma|Gastrointestinal Stromal Tumor|Paraganglioma Other: Laboratory Biomarker Analysis|Drug: Linsitinib|Other: Pharmacological Study National Cancer Institute (NCI) Phase 2 2012-03-01 2016-11-18

    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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