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Rucaparib phosphate

AG-014699 phosphate,PF-01367338 phosphate

Rucaparib phosphate是PARP抑制剂，对PARP1的Ki为1.4 nM，对PARP其余亚型也有亲和性。

目录号
EY0972
EY0972
EY0972
纯度
99.35%
99.35%
99.35%
规格
5 mg
10 mg
50 mg
原价
729.00_
1,260.00_
2996.00_
售价
729.00_
1,260.00_
2996.00_
库存
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Rucaparib phosphate is a potent PARP inhibitor with Ki of 1.4 nM.

  • 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

    0.4 μM

  • 动物实验

    1 mg/kg 腹腔注射，每天1次或4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] Thomas HD, et al. Mol Cancer Ther, 2007, 6(3), 945-956.
    [2] Daniel RA, et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. Br J Cancer, 2010, 103(10), 1588-1596.
    [3] Daniel RA, et al. Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15(4), 1241-1249.

    分子式
    C19H21FN3O5P    		 分子量
    421.36    		 CAS号
    459868-92-9    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    85 mg/mL    		 Water
    100 mM    		 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
    NCT02986100 Solid Tumor Drug: C-14 labeled Rucaparib|Drug: Rucaparib Clovis Oncology, Inc. Phase 1 2016-11-01 2017-03-16
    NCT02855944 Ovarian Cancer|Epithelial Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer Drug: Chemotherapy|Drug: Rucaparib Clovis Oncology, Inc.|Foundation Medicine Phase 3 2016-09-01 2017-03-06
    NCT02952534 Metastatic Castration Resistant Prostate Cancer Drug: Rucaparib Clovis Oncology, Inc.|Foundation Medicine Phase 2 2016-11-01 2017-03-17
    NCT01482715 Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer|Advanced Solid Tumor With Evidence of Germline or Somatic BRCA Drug: Rucaparib Clovis Oncology, Inc. Phase 1|Phase 2 2011-11-01 2016-07-05
    NCT02042378 Pancreatic Cancer|Pancreatic Ductal Adenocarcinoma Drug: Rucaparib Clovis Oncology, Inc. Phase 2 2014-04-01 2016-06-16
    NCT01891344 Ovarian Cancer|Epithelial Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer Drug: Oral rucaparib Clovis Oncology, Inc.|Foundation Medicine Phase 2 2013-09-01 2016-07-05
    NCT02505048 Metastatic Breast Cancer Drug: rucaparib UNICANCER|Clovis Oncology, Inc.|Fondation ARC Phase 2 2016-03-01 2017-02-09
    NCT01968213 Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer Drug: Rucaparib|Drug: Placebo Clovis Oncology, Inc. Phase 3 2014-01-01 2016-07-05
    NCT02975934 Metastatic Castration Resistant Prostate Cancer Drug: Rucaparib|Drug: Abiraterone acetate or Enzalutamide or Docetaxel Clovis Oncology, Inc.|Foundation Medicine Phase 3 2017-01-01 2017-02-16
    NCT02740712 Neoplasms Drug: Caffeine|Drug: Warfarin|Drug: Omeprazole|Drug: Midazolam|Drug: digoxin|Drug: Vitamin K|Drug: Rucaparib Clovis Oncology, Inc. Phase 1 2016-03-01 2017-03-01
    NCT01009190 Advanced Solid Tumors Drug: PF-01367338|Drug: Carboplatin|Drug: PF-01367338|Drug: Carboplatin Clovis Oncology, Inc. Phase 1 2010-02-01 2015-07-28
    NCT00664781 brca1 Mutation Carrier|brca2 Mutation Carrier|Breast Cancer|Ovarian Cancer Drug: rucaparib (CO-338; formally AG-014699 or PF-01367338)|Genetic: protein expression analysis|Genetic: western blotting|Other: immunohistochemistry staining method|Other: liquid chromatography|Other: mass spectrometry|Other: pharmacological study Cancer Research UK Phase 2 2007-12-01 2016-05-23
    NCT00457470 Diabetes Mellitus|Diabetic Retinopathy Drug: AG-014699 Pfizer Phase 2 2007-06-01 2015-04-30
    NCT01074970 Breast Cancer Drug: Cisplatin|Drug: Rucaparib|Drug: Cisplatin Hoosier Cancer Research Network|Clovis Oncology, Inc. Phase 2 2010-02-01 2016-08-22

    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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