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Enzastaurin

恩扎妥林,因扎妥雷,LY317615

Enzastaurin (LY317615)是PKCβ选择性抑制剂，IC50为6 nM，比对PKCα，PKCγ和PKCε的抑制性强6-20倍。

目录号
EY1694
EY1694
EY1694
EY1694
纯度
99.23%
99.23%
99.23%
99.23%
规格
5 mg
10 mg
50 mg
100 mg
原价
535
860
2310
3396
售价
535
860
2310
3396
库存
现货
现货
现货
现货
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  • 生物活性

    Enzastaurin (LY317615) is a potent and selective inhibitor of PKCβ with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Enzastaurin suppresses angiogenesis and was advanced for clinical development based upon this antiangiogenic activity.

  • 体外研究

  • 体内研究

    15% Captisol

  • 激酶实验

  • 细胞实验

    0.3-4 μM

  • 动物实验

    75 mg/kg，每天两次饲喂处理

  • 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] Graff et al (2005) The protein kinase Cβ-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. Cancer Res. 65 7462.
    [2] Teicher et al (2001) Antiangiogenic and antitumor effects of a protein kinase Cβ inhibitor in human HT-29 colon carcinoma and human CaKi1 renal cell carcinoma xenografts. Anticancer Res. 21 3175.

    分子式
    C32H29N5O2    		 分子量
    515.61    		 CAS号
    170364-57-5    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    30 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
    NCT01432951 Solid Tumor|Lymphoma, Malignant Drug: Enzastaurin Eli Lilly and Company Phase 1 2011-11-01 2017-02-14
    NCT00452413 Non-Small Cell Lung Cancer|Malignant Solid Tumor Drug: enzastaurin|Drug: erlotinib Eli Lilly and Company Phase 1|Phase 2 2007-05-01 2016-11-30
    NCT00309140 Neoplasms|Cancer Drug: enzastaurin Eli Lilly and Company Phase 2 2006-03-01 2010-05-27
    NCT00475644 Lymphoma, Follicular Drug: enzastaurin Eli Lilly and Company Phase 2 2007-05-01 2015-03-17
    NCT00088205 Mantle-Cell Lymphoma Drug: enzastaurin Eli Lilly and Company Phase 2 2004-03-01 2009-10-05
    NCT00414960 Lung Cancer Drug: enzastaurin|Drug: placebo Eli Lilly and Company Phase 2 2006-11-01 2011-02-25
    NCT00452257 Leukemia, Lymphocytic Drug: enzastaurin Eli Lilly and Company Phase 1 2007-05-01 2009-03-18
    NCT00451555 Breast Cancer Drug: enzastaurin|Drug: placebo|Drug: fulvestrant Eli Lilly and Company Phase 2 2007-03-01 2016-11-30
    NCT01388335 Solid Tumor|Lymphoma, Malignant Drug: warfarin|Drug: enzastaurin Eli Lilly and Company Phase 1 2011-08-01 2012-12-17
    NCT00503724 Brain and Central Nervous System Tumors|Neuroblastoma Drug: enzastaurin hydrochloride Pediatric Brain Tumor Consortium|National Cancer Institute (NCI) Phase 1 2007-06-01 2012-03-02
    NCT00509821 Glioblastoma Multiforme Drug: enzastaurin|Radiation: radiation Eli Lilly and Company Phase 2 2007-10-01 2016-04-22
    NCT00295815 Glioblastoma Drug: enzastaurin|Drug: lomustine Eli Lilly and Company Phase 3 2006-01-01 2016-11-21
    NCT00415363 Non Small Cell Lung Cancer|Small Cell Lung Cancer Drug: enzastaurin|Drug: placebo Eli Lilly and Company Phase 2 2006-12-01 2011-04-05
    NCT00386087 Breast Neoplasms Drug: Enzastaurin Hydrochloride Eli Lilly and Company Phase 2 2006-11-01 2008-06-05
    NCT00192114 Colonic Neoplasms Drug: Enzastaurin HCl Eli Lilly and Company Phase 2 2005-08-01 2009-10-05
    NCT00105092 Non-Small-Cell Lung Carcinoma Drug: Enzastaurin HCL Eli Lilly and Company Phase 2 2005-03-01 2007-04-27
    NCT00420381 Ovarian Cancer|Neoplasms|Carcinoma Drug: enzastaurin Eli Lilly and Company|Gynecologic Oncology Group Phase 2 2007-01-01 2015-03-10
    NCT00466440 Prostate Cancer Drug: enzastaurin|Drug: placebo|Drug: docetaxel|Drug: prednisone Eli Lilly and Company Phase 2 2007-06-01 2010-11-23
    NCT00428714 Prostate Cancer Drug: enzastaurin Eli Lilly and Company Phase 2 2007-01-01 2011-08-01
    NCT00108056 Glioma Drug: Enzastaurin (LY317615) monohydronchloride National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 1 2005-04-07 2017-01-24
    NCT00530621 Non-small Cell Lung Cancer Drug: enzastaurin|Drug: placebo|Drug: pemetrexed Eli Lilly and Company Phase 2 2007-09-01 2009-10-16
    NCT00332202 Non Hodgkin Lymphoma Drug: enzastaurin|Drug: placebo Eli Lilly and Company Phase 3 2006-06-01 2013-10-30
    NCT00586508 Recurrent Glioblastoma Drug: enzastaurin|Drug: bevacizumab Eli Lilly and Company|Genentech, Inc. Phase 2 2007-11-01 2014-01-07

    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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