Birinapant为二价Smac类似物,是XIAP和cIAP1的拮抗剂,Kd分别为45 nM和<1 nM。
Birinapant (formerly TL32711) is a Smac mimetic acts as antagonist to cIAP1 and cIAP2.
15% Captisol
1 nM-1 μM
30 mg/kg 每周腹腔注射3次
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。
[1] Allensworth JL, et al. Breast Cancer Res Treat, 2013, 137(2), 359-371.
分子式 C42H56F2N8O6 |
分子量 806.94 |
CAS号 1260251-31-7 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mg/mL |
Water <1 mg/mL |
Ethanol 50 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02587962 | Solid Tumors | Drug: Birinapant|Drug: Pembrolizumab | TetraLogic Pharmaceuticals|Merck Sharp & Dohme Corp. | Phase 1|Phase 2 | 2017-02-01 | 2016-10-18 |
NCT02147873 | Myelodysplastic Syndrome (MDS)|Chronic Myelomonocytic Leukemia (CMML) | Drug: birinapant|Drug: Azacitidine|Drug: Placebo | TetraLogic Pharmaceuticals | Phase 2 | 2014-06-01 | 2016-10-18 |
NCT01940172 | Relapsed Epithelial Ovarian Cancer|Relapsed Primary Peritoneal Cancer|Relapsed Fallopian Tube Cancer | Drug: Birinapant|Drug: Conatumumab | TetraLogic Pharmaceuticals | Phase 1 | 2013-11-01 | 2016-01-13 |
NCT01828346 | Myelodysplastic Syndrome | Drug: Birinapant|Drug: 5-Azacitidine | TetraLogic Pharmaceuticals | Phase 1|Phase 2 | 2013-06-01 | 2016-04-19 |
NCT01188499 | Cancer | Drug: Birinapant | TetraLogic Pharmaceuticals | Phase 1|Phase 2 | 2010-10-01 | 2016-04-21 |
NCT02288208 | Hepatitis B | Drug: Antiviral Therapy (tenofovir or entecavir)|Drug: Birinapant|Drug: Placebo (for birinapant) | TetraLogic Pharmaceuticals | Phase 1 | 2014-11-01 | 2016-02-04 |
NCT02756130 | Advanced Newly Diagnosed or Recurrent High Grade Serous Carcinomas (HGSC) | Drug: Birinapant|Drug: Paclitaxel|Drug: Carboplatin | Jonsson Comprehensive Cancer Center|TetraLogic Pharmaceuticals | Phase 2 | 2017-01-01 | 2017-01-20 |
NCT01681368 | Epithelial Ovarian Cancer|Peritoneal Neoplasms|Fallopian Tube Neoplasms | Drug: Birinapant (TL32711) | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | Phase 2 | 2012-08-01 | 2015-10-14 |
NCT00993239 | Cancer | Drug: Birinapant (TL32711) | TetraLogic Pharmaceuticals | Phase 1 | 2009-11-01 | 2016-03-01 |
NCT01573780 | Unspecified Adult Solid Tumor, Protocol Specific | Drug: Smac mimetic TL32711|Drug: gemcitabine hydrochloride|Other: laboratory biomarker analysis|Other: pharmacological study|Procedure: biopsy | Roswell Park Cancer Institute|National Cancer Institute (NCI)|TetraLogic Pharmaceuticals | Phase 1 | 2012-04-01 | 2014-01-14 |
NCT01766622 | Ovarian Neoplasms|Ovarian Cancer|Fallopian Tube Neoplasms|Fallopian Tube Cancer | Drug: [18F]-CP18|Procedure: PET/ CT | National Institutes of Health Clinical Center (CC)|National Cancer Institute (NCI) | Phase 2 | 2012-11-30 | 2017-01-24 |
NCT01486784 | Acute Myelogenous Leukemia | Drug: TL32711 | Abramson Cancer Center of the University of Pennsylvania | Phase 1|Phase 2 | 2011-11-01 | 2017-01-24 |
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。
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