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R428

BGB324

R428是Axl抑制剂，IC50为14 nM。

目录号
EY1287
EY1287
EY1287
EY1287
纯度
99.25%
99.25%
99.25%
99.25%
规格
2 mg
5 mg
10 mg
50 mg
原价
810
1300
2300
4400
售价
810
1300
2300
4400
库存
现货
现货
现货
现货
订购
订购
订购
订购
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  • 生物活性

    R428 is a potent and selective small-molecule inhibitor of Axl kinase with IC50 of 14 nM.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0.03, 0.3, 3 μM

  • 动物实验

    125 mg/kg 口服，一天两次

  • 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] Holland SJ, et al. Cancer Res, 2010, 70(4), 1544-1554.

    分子式
    C30H34N8    		 分子量
    506.64    		 CAS号
    1037624-75-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    5 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
    NCT01811056 Termination of Pregnancy Drug: Mifepristone Gynuity Health Projects 2013-04-01 2015-08-11
    NCT00832871 Cancer Drug: Mifepristone New Mexico Cancer Care Alliance|The Feminist Majority Foundation 2008-11-01 2016-06-22
    NCT01224509 Cervical Prostaglandin EP3 Receptors|Pregnancy Drug: Mifepristone|Other: Non-treatment University of Southern California 2004-09-01 2010-10-19
    NCT00712595 Uterine Fibroids Drug: Mifepristone|Drug: Mifepristone Mediterranea Medica S. L. Phase 2|Phase 3 2007-01-01 2009-04-22
    NCT00936741 Cushing's Syndrome Drug: mifepristone Corcept Therapeutics Phase 3 2009-07-01 2014-02-19
    NCT01990560 Mild Hypercortisolism Drug: Mifepristone Icahn School of Medicine at Mount Sinai Phase 4 2013-11-01 2016-09-29
    NCT00140478 Prostate Cancer|Adenocarcinoma of Prostate Drug: Mifepristone Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Massachusetts General Hospital|Brigham and Women's Hospital|Georgetown University Phase 2 2005-02-01 2009-12-07
    NCT02642939 Non-Small Cell Lung Cancer (NSCLC) Drug: Mifepristone Check, Jerome H., M.D., Ph.D.|Corcept Therapeutics Phase 2 2015-12-01 2016-12-12
    NCT00886873 Uterine Fibroids Drug: Mifepristone Mediterranea Medica S. L. Phase 2|Phase 3 2008-05-01 2014-10-16
    NCT01786226 Uterine Fibroids Drug: Oral administration of mifepristone 2.5 mg daily for three months|Drug: Oral administration of mifepristone 5 mg daily for three months Mediterranea Medica S. L. Phase 2|Phase 3 2010-03-01 2014-09-04
    NCT01925092 Cushing's Disease Drug: mifepristone Corcept Therapeutics|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) Phase 3 2013-08-01 2014-07-31
    NCT02720991 Abortion, 3 Months Drug: Mifepristone|Drug: Sublingual misoprostol Gynuity Health Projects|Hopital La Rabta Phase 4 2014-07-01 2016-03-22
    NCT00177372 Anembryonic Pregnancy|Gestation Abnormality|Intrauterine Fetal Demise Term Drug: mifepristone/misoprostol University of Pittsburgh Phase 4 2005-01-01 2016-01-28
    NCT00133705 Leiomyoma Drug: Mifepristone|Drug: Inert Capsule University of Rochester|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) Phase 3 2003-07-01 2014-02-13
    NCT01134198 Cocaine Dependence Drug: Mifepristone|Drug: placebo New York State Psychiatric Institute Phase 2|Phase 3 2010-05-01 2016-10-25
    NCT00637494 Psychotic Depression|Severe Major Depression With Psychotic Features|Psychosis Drug: mifepristone|Drug: placebo Corcept Therapeutics Phase 3 2008-03-01 2016-12-23
    NCT00505739 Endometrial Cancer Drug: Mifepristone M.D. Anderson Cancer Center Phase 2 2001-09-01 2012-07-26
    NCT01798017 Menstrual Regulation Drug: Mifepristone and misoprostol Gynuity Health Projects Phase 4 2012-11-01 2015-12-08
    NCT01371565 Cushing's Disease|Cushing's Syndrome Drug: Mifepristone Corcept Therapeutics Phase 3 2010-11-01 2014-02-19
    NCT02620904 Intrauterine Fetal Demise|Fetal Death Drug: Mifepristone|Drug: placebo Montefiore Medical Center Phase 4 2016-02-01 2016-10-14
    NCT02014337 Breast Cancer|Ovarian Epithelial Cancer Recurrent|Sarcoma|Non-small Cell Lung Cancer|Carcinoma, Transitional Cell|Prostate Cancer|Prostatic Neoplasms Drug: Mifepristone and Eribulin in combination Corcept Therapeutics Phase 1 2014-01-01 2016-12-21
    NCT00386282 Abortion, First Trimester Drug: mifepristone-misoprostol treatment Gynuity Health Projects 2006-09-01 2014-07-29
    NCT00994734 Termination of Pregnancy Drug: Mifepristone Gynuity Health Projects 2009-05-01 2012-04-16
    NCT00881140 Uterine Fibroid|Vaginal Bleeding. Drug: mifepristone vaginal tablets BioPro Medical Ltd Phase 2 2009-04-01 2012-12-18
    NCT00285818 Depression Drug: Mifepristone|Drug: Placebo Oral Capsule Stanford University 2003-01-01 2016-12-23

    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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