Home > PARP & PARP & > Talazoparib

Talazoparib

LT-673,LT 673,LT673,BMN 673,BMN-673,BMN673,

BMN 673是一种新型的PARP抑制剂,IC50为0.58 nM,也有效抑制PARP-2,但不抑制PARG,对PTEN突变型高度敏感。

目录号
EY0535
EY0535
EY0535
纯度
99.32%
99.32%
99.32%
规格
2 mg
5 mg
10 mg
原价
500
1300
1900
售价
500
1300
1900
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    0.33 mg/kg/day,每天一次口服处理

  • 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 AKm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] Wang B, et al. Molecular Cancer Therapeutics, 2009, 8 (12 Suppl), A121.

    分子式
    C19H14F2N6O
    分子量
    380.35
    CAS号
    1207456-01-6
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    35 mg/mL
    Water
    <1 mg/mL
    Ethanol
    <1 mg/mL

    体内溶解度

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

    NCT02282345 Breast Cancer Drug: Talazoparib M.D. Anderson Cancer Center|Medivation, Inc. Phase 2 2015-04-01 2017-03-16
    NCT03070548 Advanced Solid Tumors Drug: Talazoparib Medivation, Inc. Phase 1 2016-10-01 2017-02-28
    NCT01286987 Advanced or Recurrent Solid Tumors|Breast Neoplasms|Ovarian Cancer, Epithelial|Ewing Sarcoma|Small Cell Lung Carcinoma|Prostate Cancer|Pancreas Cancer Drug: Talazoparib Medivation, Inc. Phase 1 2010-12-01 2016-03-09
    NCT03042910 Solid Tumor Drug: Talazoparib Medivation, Inc. Phase 1 2016-10-01 2017-02-01
    NCT02567396 Estrogen Receptor Negative|Head and Neck Squamous Cell Carcinoma|HER2/Neu Negative|Hormone-Resistant Prostate Cancer|Metastatic Pancreatic Adenocarcinoma|Progesterone Receptor Negative|Solid Neoplasm|Stage III Mesothelioma|Stage IIIA Gastric Cancer|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Small Cell Lung Carcinoma|Stage IIIB Gastric Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Small Cell Lung Carcinoma|Stage IIIC Gastric Cancer|Stage IIIC Ovarian Cancer|Stage IV Mesothelioma|Stage IV Non-Small Cell Lung Cancer|Stage IV Ovarian Cancer|Stage IV Small Cell Lung Carcinoma|Triple-Negative Breast Carcinoma Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Talazoparib National Cancer Institute (NCI) Phase 1 2016-07-01 2017-02-06
    NCT02997163 Advanced Solid Tumors Drug: Talazoparib Medivation, Inc. Phase 1 2017-01-01 2016-12-15
    NCT02997176 Advanced Solid Tumors Drug: Talazoparib Medivation, Inc. Phase 1 2016-11-01 2016-12-15
    NCT02286687 Advanced Cancers Drug: Talazoparib Tosylate|Behavioral: Phone Call M.D. Anderson Cancer Center|BioMarin Pharmaceutical Phase 2 2014-12-22 2017-02-06
    NCT02401347 Advanced Breast Cancer|HER2/Neu Negative|Triple-Negative Breast Cancer Drug: Talazoparib Tosylate Melinda Telli|National Cancer Institute (NCI)|Stanford University Phase 2 2015-08-01 2015-08-09
    NCT02034916 Breast Neoplasms|BRCA 1 Gene Mutation|BRCA 2 Gene Mutation Drug: talazoparib Medivation, Inc.|Myriad Genetic Laboratories, Inc. Phase 2 2014-01-01 2016-12-13
    NCT02836028 Ovarian Cancer Drug: Talazoparib|Drug: Temozolomide Medivation, Inc.|Myriad Genetic Laboratories, Inc. Phase 2 2016-10-01 2016-12-20
    NCT02878785 Acute Myeloid Leukemia Drug: Decitabine|Drug: talazoparib University of Maryland|Medivation, Inc. Phase 1|Phase 2 2016-08-01 2016-08-21
    NCT02627430 Adult Solid Neoplasm|Estrogen Receptor Negative|Fallopian Tube Serous Neoplasm|HER2/Neu Negative|Ovarian Serous Adenocarcinoma|Ovarian Serous Tumor|Primary Peritoneal Serous Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma Drug: Hsp90 Inhibitor AT13387|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Talazoparib National Cancer Institute (NCI) Phase 1 2016-03-01 2016-07-22
    NCT02392793 Childhood Solid Tumors Drug: Talazoparib|Drug: Irinotecan|Drug: Temozolomide|Drug: Filgrastim|Drug: Peg-filgrastim St. Jude Children's Research Hospital|BioMarin Pharmaceutical|Alliance Pharma|Pfizer Phase 1 2015-03-16 2017-02-08
    NCT02921919 Cancer Drug: Talazoparib Medivation, Inc. Phase 2 2016-09-01 2017-01-31
    NCT02317874 Solid Neoplasm Drug: Carboplatin|Other: Laboratory Biomarker Analysis|Drug: Paclitaxel|Other: Pharmacological Study|Drug: Talazoparib National Cancer Institute (NCI) Phase 1 2015-07-01 2017-03-22
    NCT01945775 Breast Neoplasms|BRCA 1 Gene Mutation|BRCA 2 Gene Mutation Drug: talazoparib|Drug: Physician's-Choice Medivation, Inc. Phase 3 2013-10-01 2016-12-08
    NCT02537561 Solid Tumors|Carcinoma, Non-Small Cell Lung|Non-Small Cell Lung Cancer|Non-Small-Cell Lung Carcinoma|Nonsmall Cell Lung Cancer Drug: Cisplatin|Drug: Gemcitabine|Drug: Talazoparib Washington University School of Medicine|BioMarin Pharmaceutical Phase 1 2015-12-01 2016-02-10
    NCT02116777 Adult Solid Neoplasm|Childhood Solid Neoplasm|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Lymphoblastic Leukemia|Recurrent Childhood Central Nervous System Neoplasm|Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Refractory Central Nervous System Neoplasm Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Talazoparib|Drug: Temozolomide National Cancer Institute (NCI) Phase 1|Phase 2 2014-05-01 2017-03-22
    NCT02316834 Fallopian Tube Cancer|Ovarian Cancer|Peritoneal Cancer Drug: BMN 673 M.D. Anderson Cancer Center|BioMarin Pharmaceutical|National Cancer Institute (NCI) Early Phase 1 2015-06-01 2017-02-24

    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。

  • 相关化合物库

  • 使用AMQUAR产品发表文献后请联系我们

相关推荐

X
  • 联系人 :
  • 收件地址 :
  • 电话号码 :
  • 单位名称 :
  • 产品货号 :
  • 产品规格 :
  • 发票抬头以及单位税号 :