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SKI II

SKI II是一种高度选择性的，非ATP竞争性的S1P receptor抑制剂，IC50为0.5 μM，对其他激酶，包括PI3K， PKCα和ERK2没有抑制作用。

目录号
EY0309
EY0309
EY0309
EY0309
EY0309
纯度
99.61%
99.61%
99.61%
99.61%
99.61%
规格
1 mg
5 mg
10 mg
25 mg
50 mg
原价
220
480
660
1060
1900
售价
220
480
660
1060
1900
库存
现货
现货
现货
现货
现货
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  • 生物活性

    SKI II is a highly selective and non ATP-competitive S1P receptor inhibitor with IC50 of 0.5 μM, while exhibiting no inhibitory action on other kinases including PI3K, PKCα and ERK2.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~50 μM

  • 动物实验

    ~100 mg/kg 腹腔给药或口服给药

  • 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] French KJ, et al. Cancer Res, 2003, 63(18), 5962-5969.
    [2] Zu-An Zhu et. Al. Reversion of multidrug resistance by SKI-II in SGC7901/DDP cells and exploration of underlying mechanisms. Asian Pacific journal of cancer prevention : APJCP, 13(2), 625-631 (2012).
    [3] Kyong-Oh Shin et. Al. Ginsenoside compound K inhibits angiogenesis via regulation of sphingosine kinase-1 in human umbilical vein endothelial cells. Archives of Pharmacal Research, 37(9), 1183-1192 (2014).
    [4] Jingjing Ge et. Al. Essential Roles of RNA-binding Protein HuR in Activation of Hepatic Stellate Cells Induced by Transforming Growth Factor-β1. Scientific reports, 6, 22141 (2016).

    分子式
    C15H11ClN2OS    		 分子量
    302.78    		 CAS号
    312636-16-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mM    		 Water
    <1 mg/mL    		 Ethanol
    75 mM

    体内溶解度

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

    NCT02079675 Non-constipation Irritable Bowel Syndrome Drug: SKI3246 Low Dose|Drug: SKI3246 High Dose|Drug: Placebo SK Chemicals Co.,Ltd. Phase 2 2013-01-01 2015-05-29
    NCT02311998 Leukemia Drug: Bosutinib|Drug: Inotuzumab Ozogamicin|Behavioral: Phone Call M.D. Anderson Cancer Center|Pfizer Phase 1|Phase 2 2015-04-01 2017-02-16
    NCT00319254 Breast Neoplasms|Neoplasm Metastasis Drug: SKI-606 (Bosutinib) Pfizer Phase 2 2006-05-01 2012-12-21
    NCT02782403 Leukemia Drug: Axitinib|Drug: Bosutinib M.D. Anderson Cancer Center|Pfizer Phase 1|Phase 2 2017-03-20 2017-03-20
    NCT02906696 Chronic Myelogenous Leukemia Drug: Bosutinib|Behavioral: Phone Calls|Behavioral: Questionnaires M.D. Anderson Cancer Center|Pfizer Phase 2 2016-10-01 2017-03-01
    NCT01229969 Falls, Accidental Other: Wii Fit Balance Games|Other: NeuroCom EquiTest庐 System Atlanta VA Medical Center|Emory University 2009-08-01 2013-01-23
    NCT02251470 Stroke Other: HBE Wii (EG)|Other: HBE Control (CG) Martin-Luther-Universit盲t Halle-Wittenberg Phase 1|Phase 2 2014-10-01 2015-12-01
    NCT02728843 Parkinson's Disease Drug: Deferiprone|Drug: Placebo ApoPharma Phase 2 2016-07-01 2017-03-01
    NCT00734292 Mild to Moderate Asthma Drug: fluticasone propionate, formoterol fumarate|Other: fluticasone propionate, formoterol fumarate|Other: fluticasone propionate, formoterol fumarate SkyePharma AG|Abbott Phase 2 2008-09-01 2010-08-24
    NCT02164916 Colorectal Cancer Biological: cetuximab|Drug: irinotecan hydrochloride|Drug: vemurafenib Southwest Oncology Group|National Cancer Institute (NCI)|Genentech/Roche Phase 2 2014-11-01 2017-02-23
    NCT02965378 Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma Drug: FGFR Inhibitor AZD4547|Other: Laboratory Biomarker Analysis Southwest Oncology Group|National Cancer Institute (NCI) Phase 2|Phase 3 2014-06-01 2016-11-14
    NCT02785913 Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma Other: Laboratory Biomarker Analysis|Drug: Taselisib Southwest Oncology Group|National Cancer Institute (NCI) Phase 2 2014-06-01 2017-01-31
    NCT02785939 Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma Other: Laboratory Biomarker Analysis|Drug: Palbociclib Southwest Oncology Group|National Cancer Institute (NCI) Phase 2|Phase 3 2014-06-01 2017-01-31
    NCT01216683 Lymphoma Biological: rituximab|Drug: bendamustine hydrochloride|Drug: bortezomib|Drug: lenalidomide Eastern Cooperative Oncology Group|National Cancer Institute (NCI) Phase 2 2010-12-01 2015-03-13
    NCT01856192 CD20 Positive|Stage II Diffuse Large B-Cell Lymphoma|Stage III Diffuse Large B-Cell Lymphoma|Stage IV Diffuse Large B-Cell Lymphoma Drug: Cyclophosphamide|Drug: Doxorubicin Hydrochloride|Other: Laboratory Biomarker Analysis|Drug: Lenalidomide|Drug: Prednisone|Biological: Rituximab|Drug: Vincristine Sulfate National Cancer Institute (NCI) Phase 2 2013-08-01 2017-03-23
    NCT00853580 Neurofibromatosis Type 1 Drug: Lovastatin 鈩Device: placebo University of Alabama at Birmingham|Boston Children鈥檚 Hospital|Children's Hospital of Philadelphia|Children's Research Institute|Children's Hospital Medical Center, Cincinnati|National Cancer Institute (NCI)|University of Chicago|University of Utah|Washington University School of Medicine|Sydney Children's Network|University of Texas Southwestern Medical Center Phase 2 2009-07-01 2016-12-02
    NCT01642251 Extensive Stage Small Cell Lung Carcinoma|Large Cell Lung Carcinoma|Neuroendocrine Carcinoma|Small Cell Carcinoma|Stage IV Non-Small Cell Lung Cancer Drug: Cisplatin|Drug: Etoposide|Other: Laboratory Biomarker Analysis|Other: Placebo|Other: Quality-of-Life Assessment|Other: Questionnaire Administration|Drug: Veliparib National Cancer Institute (NCI) Phase 1|Phase 2 2012-09-01 2017-03-23
    NCT00217737 Colon Mucinous Adenocarcinoma|Colon Signet Ring Cell Adenocarcinoma|Lynch Syndrome|Stage IIA Colon Cancer|Stage IIB Colon Cancer|Stage IIC Colon Cancer Biological: Bevacizumab|Drug: Fluorouracil|Other: Laboratory Biomarker Analysis|Drug: Leucovorin Calcium|Drug: Oxaliplatin National Cancer Institute (NCI) Phase 3 2005-08-01 2016-12-30
    NCT00003641 Melanoma (Skin) Biological: interferon alfa-2b|Other: observation ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Southwest Oncology Group|Cancer and Leukemia Group B|NCIC Clinical Trials Group|Children's Oncology Group|Eastern Cooperative Oncology Group Phase 3 1998-12-01 2016-03-31
    NCT00324805 Stage IB Non-Small Cell Lung Carcinoma|Stage IIA Non-Small Cell Lung Carcinoma|Stage IIB Non-Small Cell Lung Carcinoma|Stage IIIA Non-Small Cell Lung Cancer Biological: Bevacizumab|Drug: Cisplatin|Drug: Docetaxel|Drug: Gemcitabine Hydrochloride|Other: Laboratory Biomarker Analysis|Drug: Pemetrexed Disodium|Other: Questionnaire Administration|Drug: Vinorelbine Tartrate National Cancer Institute (NCI)|Cancer and Leukemia Group B|NCIC Clinical Trials Group|North Central Cancer Treatment Group|Southwest Oncology Group Phase 3 2007-06-01 2017-03-23

    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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