Home > Kinesin & Kinesin & > Ispinesib

Ispinesib

伊斯平斯,CK0238273,CK 0238273,CK-0238273,SB715992,SB 715992,SB-715992,

Ispinesib是一种有效的，特异性的，可逆的kinesin spindle protein (KSP)（纺锤体驱动蛋白）抑制剂，Kiapp为1.7 nM，对CENP-E， RabK6， MCAK， MKLP1， KHC和Kif1A没有抑制作用。

目录号
EY1017
EY1017
EY1017
EY1017
纯度
99.55%
99.55%
99.55%
99.55%
规格
1 mg
5 mg
10 mg
50 mg
原价
280
780
1200
4100
售价
280
780
1200
4100
库存
现货
现货
现货
现货
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  • 生物活性

    Ispinesib (SB-715992) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Phase 2.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0.085 nM-33 μM

  • 动物实验

    10 mg/kg作用于裸鼠，8 mg/kg作用于SCID 鼠3倍剂量腹腔注射，每隔四天进行一次

  • 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] Lad L, et al. Biochemistry, 2008, 47(11), 3576-3585.

    分子式
    C30H33ClN4O2    		 分子量
    517.06    		 CAS号
    336113-53-2    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    200 mM    		 Water
    <1 mg/mL    		 Ethanol
    200 mM

    体内溶解度

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

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00354250 Recurrent Renal Cell Cancer|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer Drug: ispinesib National Cancer Institute (NCI) Phase 2 2006-05-01 2013-06-04
    NCT00119171 Solid Tumor Cancer Drug: Ispinesib|Drug: Capecitabine GlaxoSmithKline Phase 1 2004-11-01 2008-10-15
    NCT00136578 Solid Tumor Cancer Drug: Ispinesib|Drug: carboplatin GlaxoSmithKline Phase 1 2004-10-01 2008-10-15
    NCT00095628 Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma|Recurrent Metastatic Squamous Neck Cancer With Occult Primary|Recurrent Salivary Gland Cancer|Recurrent Squamous Cell Carcinoma of the Hypopharynx|Recurrent Squamous Cell Carcinoma of the Larynx|Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity|Recurrent Squamous Cell Carcinoma of the Oropharynx|Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity|Recurrent Verrucous Carcinoma of the Larynx|Recurrent Verrucous Carcinoma of the Oral Cavity|Stage IV Squamous Cell Carcinoma of the Hypopharynx|Stage IV Squamous Cell Carcinoma of the Larynx|Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity|Stage IV Squamous Cell Carcinoma of the Oropharynx|Stage IV Verrucous Carcinoma of the Larynx|Stage IV Verrucous Carcinoma of the Oral Cavity|Stage IVA Salivary Gland Cancer|Stage IVA Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity|Stage IVB Salivary Gland Cancer|Stage IVB Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity|Stage IVC Salivary Gland Cancer|Stage IVC Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity Drug: ispinesib|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 2 2005-01-01 2017-01-13
    NCT00089973 Breast Cancer Drug: Ispinesib GlaxoSmithKline Phase 2 2004-06-01 2010-10-01
    NCT00097409 Ovarian Cancer Drug: Ispinesib GlaxoSmithKline Phase 2 2004-12-01 2010-10-01
    NCT00363272 Childhood Burkitt Lymphoma|Childhood Central Nervous System Germ Cell Tumor|Childhood Choroid Plexus Tumor|Childhood Craniopharyngioma|Childhood Grade I Meningioma|Childhood Grade II Meningioma|Childhood Grade III Meningioma|Childhood High-grade Cerebral Astrocytoma|Childhood Infratentorial Ependymoma|Childhood Low-grade Cerebral Astrocytoma|Childhood Spinal Cord Neoplasm|Childhood Supratentorial Ependymoma|Recurrent Childhood Brain Stem Glioma|Recurrent Childhood Brain Tumor|Recurrent Childhood Cerebellar Astrocytoma|Recurrent Childhood Cerebral Astrocytoma|Recurrent Childhood Ependymoma|Recurrent Childhood Grade III Lymphomatoid Granulomatosis|Recurrent Childhood Large Cell Lymphoma|Recurrent Childhood Lymphoblastic Lymphoma|Recurrent Childhood Medulloblastoma|Recurrent Childhood Small Noncleaved Cell Lymphoma|Recurrent Childhood Supratentorial Primitive Neuroectodermal Tumor|Recurrent Childhood Visual Pathway and Hypothalamic Glioma|Unspecified Childhood Solid Tumor, Protocol Specific Drug: ispinesib|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2006-06-01 2013-01-15
    NCT00101244 Adult Grade III Lymphomatoid Granulomatosis|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Small Lymphocytic Lymphoma|Splenic Marginal Zone Lymphoma|Stage IV Adult Burkitt Lymphoma|Stage IV Adult Diffuse Large Cell Lymphoma|Stage IV Adult Diffuse Mixed Cell Lymphoma|Stage IV Adult Diffuse Small Cleaved Cell Lymphoma|Stage IV Adult Hodgkin Lymphoma|Stage IV Adult Immunoblastic Large Cell Lymphoma|Stage IV Adult Lymphoblastic Lymphoma|Stage IV Grade 1 Follicular Lymphoma|Stage IV Grade 2 Follicular Lymphoma|Stage IV Grade 3 Follicular Lymphoma|Stage IV Mantle Cell Lymphoma|Stage IV Marginal Zone Lymphoma|Stage IV Small Lymphocytic Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific|Waldenstr枚m Macroglobulinemia Drug: ispinesib|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2004-11-01 2013-01-11
    NCT00098826 Acute Undifferentiated Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Acute Promyelocytic Leukemia (M3)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|de Novo Myelodysplastic Syndromes|Previously Treated Myelodysplastic Syndromes|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Refractory Anemia With Excess Blasts|Refractory Anemia With Excess Blasts in Transformation|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia|Secondary Myelodysplastic Syndromes|Untreated Adult Acute Myeloid Leukemia Drug: ispinesib|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2004-12-01 2013-01-10
    NCT00096499 Adenocarcinoma of the Prostate|Recurrent Prostate Cancer|Stage IV Prostate Cancer Drug: ispinesib|Other: pharmacological study|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2005-04-01 2013-01-24
    NCT00085813 Non-Small-Cell Lung Cancer Drug: Ispinesib GlaxoSmithKline Phase 2 2003-12-01 2010-10-01
    NCT00095953 Melanoma (Skin) Drug: ispinesib NCIC Clinical Trials Group|National Cancer Institute (NCI) Phase 2 2004-11-01 2013-05-16
    NCT00095992 Liver Cancer Drug: ispinesib NCIC Clinical Trials Group|National Cancer Institute (NCI)|Canadian Cancer Trials Group Phase 2 2004-11-01 2011-09-26
    NCT00103311 Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IIIA Colon Cancer|Stage IIIA Rectal Cancer|Stage IIIB Colon Cancer|Stage IIIB Rectal Cancer|Stage IIIC Colon Cancer|Stage IIIC Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer Drug: ispinesib|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2005-01-01 2015-02-13
    NCT00607841 Breast Neoplasms Drug: Ispinesib (SB-715992)|Drug: Ispinesib (SB-715992) Cytokinetics Phase 1|Phase 2 2007-12-01 2010-01-14
    NCT00169520 Solid Tumor Cancer Drug: docetaxel|Drug: SB-715992 GlaxoSmithKline Phase 1 2004-06-01 2008-10-15

    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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