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Sotrastaurin

AEB071,AEB-071

Sotrastaurin(AEB-071)是PKCθ选择性抑制剂，Ki为0.22 nM。

目录号
EY0738
EY0738
EY0738
纯度
99.39%
99.39%
99.39%
规格
1 mg
5 mg
25 mg
原价
400
1000
1600
售价
400
1000
1600
库存
现货
现货
现货
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  • 生物活性

    Sotrastaurin is a potent inhibitor of novel and classical PKC isoforms. Through the inhibition of PKC, Sotrastaurin can depress the activation and proliferation of T-cell and decrease the production of cytokine.Sotrastaurin can also suppress the NK cell activity. Ex vivo stimulation of lymphocytes from subjects exposed to single doses of Sotrastaurin resulted in a dose-dependent inhibition of both lymphocyte proliferation and IL2 mRNA expression.

  • 体外研究

  • 体内研究

    生理盐水

  • 激酶实验

  • 细胞实验

  • 动物实验

    10 mg/kg 和 30 mg/kg 口服一次

  • 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] Evenou JP, et al. J Pharmacol Exp Ther, 2009, 330(3), 792-801.

    分子式
    C25H22N6O2    		 分子量
    438.48    		 CAS号
    425637-18-9    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >75 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    2 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
    NCT02285244 Prolymphocytic Leukemia|Recurrent Mantle Cell Lymphoma|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Richter Syndrome Drug: sotrastaurin acetate|Other: pharmacological study|Other: laboratory biomarker analysis James Blachly|Novartis|Ohio State University Comprehensive Cancer Center Phase 2 null 2015-03-16
    NCT02273219 Uveal Melanoma Drug: AEB071|Drug: BYL719 Richard D. Carvajal|Columbia University Phase 1 2014-11-01 2016-12-15
    NCT01064791 Renal Transplantation Drug: sotrastaurin (Dose 1) + tacrolimus + standard of care medications|Drug: sotrastaurin (Dose 2) + tacrolimus + standard of care medications|Drug: sotrastaurin (Dose 3) + tacrolimus + standard of care medications|Drug: mycophenolic acid + tacrolimus + standard of care medications Novartis Pharmaceuticals|Novartis Phase 2 2009-12-01 2016-11-16
    NCT00545259 de Novo Liver Transplantation Drug: AEB071 Novartis Phase 1 2007-10-01 2011-04-08
    NCT01801358 Uveal Melanoma Drug: AEB071|Drug: MEK162 Array BioPharma Phase 1|Phase 2 2013-08-01 2016-08-29
    NCT00504543 Kidney Transplantation Drug: AEB071|Drug: Certican|Drug: Neoral Novartis Pharmaceuticals|Novartis Phase 2 2007-07-01 2016-11-16
    NCT01128335 Liver Transplantation Drug: MMF(1000mg bid) + tacrolimus + standard of care medications|Drug: sotrastaurin (200mg bid) + tacrolimus + standard of care medications|Drug: sotrastaurin (200mg bid) + tacrolimus + standard of care medications|Drug: sotrastaurin (300 mg bid) + tacrolimus + standard of care medications Novartis Pharmaceuticals|Novartis Phase 2 2010-04-01 2016-11-17
    NCT01854606 CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma Drug: AEB071|Drug: Everolimus Novartis Pharmaceuticals|Novartis Phase 1|Phase 2 2013-12-05 2017-02-13
    NCT00409929 Healthy Drug: AEB071 Novartis Phase 1 2006-06-01 2010-10-18
    NCT01430416 Uveal Melanoma Drug: AEB071 Novartis Pharmaceuticals|Novartis Phase 1 2011-12-20 2017-02-13
    NCT01402440 Diffuse Large B-Cell Lymphoma Drug: AEB071 Novartis Pharmaceuticals|Novartis Phase 1 2011-11-01 2015-01-06
    NCT00416546 Healthy Drug: AEB071 Novartis Phase 1 2006-10-01 2008-08-08
    NCT00615693 Uveitis|Posterior Uveitis|Panuveitis Drug: AEB071 Novartis Phase 2 2008-07-01 2017-02-21
    NCT00820911 Kidney Transplantation Drug: cyclosporine (reduced exposure) / everolimus|Drug: AEB071 300 mg b.i.d. / everolimus|Drug: AEB071 200 mg b.i.d. / everolimus Novartis Pharmaceuticals|Novartis Phase 2 2008-09-01 2017-02-22
    NCT00885196 Moderate and Severe Plaque Psoriasis Drug: Placebo|Drug: AEB071 Novartis Pharmaceuticals|Novartis Phase 2 2009-04-01 2016-11-15
    NCT00572585 Ulcerative Colitis Drug: AEB071|Drug: Placebo Novartis Pharmaceuticals|Novartis Phase 2 2010-04-01 2016-09-22
    NCT00403416 Kidney Transplantation Drug: AEB071|Drug: Mycophenolic Acid Novartis Pharmaceuticals|Novartis Phase 1|Phase 2 2006-10-01 2009-02-26
    NCT00555789 Kidney Transplantation Drug: AEB071|Drug: mycophenolic plus tacrolimus Novartis Pharmaceuticals|Novartis Phase 2 2007-10-01 2012-07-31
    NCT00492869 Kidney Transplantation Drug: AEB071 Novartis Pharmaceuticals|Novartis Phase 1|Phase 2 2007-01-01 2016-09-22
    NCT01594255 Healthy Drug: sotrastaurin|Drug: sotrastaurin|Drug: placebo to sotrastaurin|Drug: Avelox Novartis Pharmaceuticals|Novartis Phase 1 2009-07-01 2012-05-07
    NCT00410228 Healthy Drug: AHT956 Novartis Phase 1 2006-06-01 2007-06-21

    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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