TIC10是口服活性的稳定化合物,能抑制Akt和ERK,能透过血脑屏障,可诱导TRAIL。
TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.
25, 50, 100 mg/kg 腹腔处理/口服处理
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] Allen JE, et al. Sci Transl Med, 2013, 5(171), 171ra17.
分子式 C24H26N4O |
分子量 386.49 |
CAS号 41276-02-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 6 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02038699 | Advanced Glioblastoma|Advanced Colorectal Cancer|Advanced Triple-negative Breast Cancer|Advanced Non-small Cell Lung Cancer | Drug: ONC201 | Oncoceutics, Inc. | Phase 1|Phase 2 | null | 2015-12-18 |
NCT02250781 | Solid Tumors | Drug: Oral ONC201 | Rutgers, The State University of New Jersey|National Cancer Institute (NCI)|Rutgers Cancer Institute of New Jersey | Phase 1 | 2015-01-01 | 2017-02-01 |
NCT02324621 | Unspecified Adult Solid Tumor | Drug: Oral ONC201|Other: pharmacological study|Other: laboratory biomarker analysis | Rutgers, The State University of New Jersey|National Cancer Institute (NCI)|Rutgers Cancer Institute of New Jersey|Oncoceutics, Inc. | Phase 1 | 2015-02-01 | 2017-01-19 |
NCT02863991 | Multiple Myeloma | Drug: ONC201 | Oncoceutics, Inc. | Phase 1|Phase 2 | 2016-01-01 | 2017-03-20 |
NCT03034200 | Recurrent Neuroendocrine Tumor|Metastatic Neuroendocrine Tumor | Drug: ONC201 | Peter Anderson|Case Comprehensive Cancer Center | Phase 2 | 2017-02-01 | 2017-01-25 |
NCT02420795 | Lymphoma | Drug: ONC201|Behavioral: Phone Call | M.D. Anderson Cancer Center|Oncoceutics, Inc. | Phase 1|Phase 2 | 2015-11-03 | 2017-01-23 |
NCT02609230 | Advanced Solid Tumors|Multiple Myeloma | Drug: ONC-201 | Fox Chase Cancer Center | Phase 1 | 2015-11-01 | 2017-01-25 |
NCT02392572 | Leukemia | Drug: ONC201 | M.D. Anderson Cancer Center|Oncoceutics, Inc. | Phase 1|Phase 2 | 2015-11-01 | 2016-12-27 |
NCT02525692 | Recurrent Glioblastoma | Drug: ONC201 | Oncoceutics, Inc. | Phase 2 | 2016-01-01 | 2017-03-19 |
NCT02190721 | Solid Tumors | Drug: tbo-filgrastim | Teva Pharmaceutical Industries | Phase 2 | 2015-05-01 | 2017-03-13 |
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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