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Plerixafor

普乐沙福,JM 3100,AMD3100

Plerixafor (AMD3100)是一种CXCR4趋化因子受体拮抗剂，抑制CXCR4和CXCL12调节的趋化性，IC50分别为44 nM和5.7 nM。

目录号
EY0683
EY0683
EY0683
EY0683
纯度
99.65%
99.65%
99.65%
99.65%
规格
5 mg
10 mg
50 mg
100 mg
原价
380
599
1600
2700
售价
380
599
1600
2700
库存
现货
现货
现货
现货
订购
订购
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  • 生物活性

    CXCR4 and SDF-1 are key factors in regulating cancer cell invasion and metastasis, and plerixafor can prevent the binding of SDF-1 to CXCR4 for inhibiting cancer metastasis. Plerixafor interfered with CXCL12/CXCR4 mediated retention of hematopoietic stem cells in the bone marrow, and resulted in their mobilization to the blood. Plerixafor amplified the release of circulating neutrophils from the oriented area in the lung, while simultaneously preventing neutrophil returned to the bone marrow. Three adults with WHIM syndrome were subcutaneously injected 0.01 to 0.02 mg/kg plerixafor twice daily for 6 months, circulating leukocytes were constantly increased, and associated with fewer infections.

  • 体外研究

  • 体内研究

    30% Propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)

  • 激酶实验

  • 细胞实验

  • 动物实验

    5 mg/kg Administered via i.p.

  • 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] Zabel BA, et al. J Immunol. 2009, 183(5), 3204-3211.

    分子式
    C28H54N8    		 分子量
    502.78    		 CAS号
    110078-46-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    <1 mg/mL    		 Water
    3 mg/mL     		Ethanol
    110 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
    NCT01149863 Autologous Transplantation Drug: Plerixafor Emory University|Genzyme, a Sanofi Company Phase 2 2010-06-01 2013-11-19
    NCT01319864 Relapsed/Refractory AML|Relapsed/Refractory ALL|Secondary AML/MDS|Acute Leukemia of Ambiguous Lineage|AML|ALL Drug: Plerixafor Dose Escalation Seattle Children's Hospital|Children's Healthcare of Atlanta|Pediatric Oncology Experimental Therapeutics Investigation Consortium Phase 1 2011-03-01 2016-10-17
    NCT01042717 Multiple Myeloma|Non-Hodgkins Lymphoma Drug: Plerixafor Shi, Patricia, M.D.|Genzyme, a Sanofi Company 2010-02-01 2011-09-26
    NCT01141543 Acute Myeloid Leukemia Drug: Plerixafor (mozobil) University Health Network, Toronto|Princess Margaret Hospital, Canada 2010-05-01 2014-07-16
    NCT01455025 Acute Myeloid Leukemia Drug: Plerixafor granulocyte-colony stimulating factor French Innovative Leukemia Organisation|Acute Leukemia French Association|Genzyme, a Sanofi Company Phase 1 2012-01-01 2016-03-15
    NCT01280955 Failure of Bone Marrow Graft Drug: Plerixafor Mitchell Horwitz, MD|Genzyme, a Sanofi Company|Duke University Phase 1|Phase 2 2011-12-01 2017-02-06
    NCT01339572 Non-Hodgkin's Lymphoma|Multiple Myeloma Drug: Plerixafor|Drug: Filgrastim University of Florida Phase 4 2011-04-01 2016-10-25
    NCT00082329 Healthy Drug: AMD 3100 (Mozobil plerixafor) Richard Childs, M.D.|National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) Phase 2 2004-05-01 2014-04-01
    NCT00694590 Chronic Lymphocytic Leukemia (CLL)|Small Lymphocytic Lymphoma (SLL) Drug: plerixafor Genzyme, a Sanofi Company|Sanofi Phase 1 2008-06-01 2015-03-19
    NCT00903968 Multiple Myeloma Drug: Plerixafor (AMD3100)|Drug: bortezomib Dana-Farber Cancer Institute|Brigham and Women's Hospital|Genzyme, a Sanofi Company|Millennium Pharmaceuticals, Inc. Phase 1|Phase 2 2009-05-01 2017-01-18
    NCT00445302 Renal Impairment Drug: plerixafor Genzyme, a Sanofi Company|Sanofi Phase 1 2006-01-01 2014-02-10
    NCT01068301 Acute Lymphoblastic Leukemia|Acute Myeloid Leukemia|Chronic Myeloid Leukemia|Myelodysplastic Syndrome|Non-Hodgkin's Lymphoma Drug: Plerixafor St. Jude Children's Research Hospital|Genzyme, a Sanofi Company Phase 1 2010-05-01 2013-12-31
    NCT00901225 Multiple Myeloma|Non-Hodgkins Lymphoma|Hodgkins Disease Drug: G-CSF plus Plerixafor Duke University|Genzyme, a Sanofi Company Phase 2 2009-05-01 2014-04-08
    NCT00990054 Acute Myeloid Leukemia Drug: Plerixafor Genzyme, a Sanofi Company|Sanofi Phase 1 2009-12-01 2015-03-19
    NCT00396331 Autologous Stem Cell Transplantation Drug: G-CSF plus plerixafor Genzyme, a Sanofi Company|Sanofi Phase 2 2005-10-01 2014-02-10
    NCT00322387 Lymphoma, Non-Hodgkin|Multiple Myeloma Drug: G-CSF and plerixafor Genzyme, a Sanofi Company|Sanofi Phase 2 2004-04-01 2014-02-10
    NCT01700608 Lymphoma|Myeloma Drug: plerixafor Fondazione IRCCS Istituto Nazionale dei Tumori, Milano 2008-09-01 2012-10-02
    NCT01696461 Related Donors Donating PBSC to a Family Member|Acute Myelogenous Leukemia|Acute Lymphoblastic Leukemia|Myelodysplastic Syndrome|Chronic Myelogenous Leukemia|Non-Hodgkin's Lymphoma|Hodgkin's Disease|Chronic Lymphocytic Leukemia Drug: Plerixafor Center for International Blood and Marrow Transplant Research|Genzyme, a Sanofi Company|Sanofi Phase 2 2013-05-01 2017-02-20
    NCT00395967 Multiple Myeloma|Lymphoma, Non-Hodgkin's Drug: G-CSF plus plerixafor Genzyme, a Sanofi Company|Sanofi Phase 2 2005-04-01 2015-04-10
    NCT00322842 Lymphoma, Non-Hodgkin|Multiple Myeloma Drug: G-CSF Plus Plerixafor Genzyme, a Sanofi Company|AnorMED|Sanofi Phase 2 2004-09-01 2014-02-10
    NCT00838357 Lymphoma (Non-Hodgkin's Lymphoma)|Hodgkin's Disease or Multiple Myeloma|Front Line Mobilization|Transplantation Drug: Generic = Plerixafor Genzyme, a Sanofi Company|Sanofi Phase 3 2008-09-01 2015-03-19

    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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