CAS No.: 1184173-73-6
MK-8353 Catalog No. CSN21082
Synonyms: SCH900353
MK-8353, also known as SCH900353, is a potent and orally active ERK1/2 inhibitor and anticancer drug candidate currently being developed by Schering-Plough. MK-8353 exhibited comparable potency with SCH772984 across various preclinical cancer models.
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纯度 & 质量文件
批次:
靶点选择性
生物活性
- 描述
- 作用机制
动物研究 剂量 Mice: 10 mg/kg[1] (i.v.); 30 mg/kg[1] (p.o.) Rat: 3 mg/kg[1] (i.v.); 30 mg/kg[1] (p.o.)
给药途径 i.v., p.o.
动物药代数据 Animal Mice[1] Rats[1] Dogs[1] Monkeys[1] Dose 10 mg/kg (i.v.)
30 mg/kg (p.o.)3 mg/kg (i.v.)
10 mg/kg (p.o.)3 mg/kg (i.v.)
30 mg/kg (p.o.)1 mg/kg (i.v.)
10 mg/kg (p.o.)Administration i.v.
p.o.i.v.
p.o.i.v.
p.o.i.v.
p.o.MRT 1.5 h (i.v.) 2.3 h (i.v.) 4.0 h (i.v.) 1.9 h (i.v.) F 80% (p.o.) 50% (p.o.) 23% (p.o.) 2% (p.o.) T1/2 1.8 h (i.v.) 1.6 h (i.v.) 2.8 h (i.v.) 1.3 h (i.v.) Tmax 1.0 h (p.o.) 1.7 h (p.o.) 4.0 h (p.o.) 1.4 h (p.o.) CL 38 ml/min/kg (i.v.) 1.0 ml/min/kg (i.v.) 3.9 ml/min/kg (i.v.) 17.9 ml/min/kg (i.v.) Cmax 4.6 μM (p.o.) 24 μM (p.o.) 6.5 μM (p.o.) 0.06 μM (p.o.) Vdss 3.3 L/kg (i.v.) 0.1 L/kg (i.v.) 0.9 L/kg (i.v.) 2.0 L/kg (i.v.) AUC0→∞ 19.4 μM·h (i.v.)
15.3 μM·h (p.o.)85 μM·h (i.v.)
143 μM·h (p.o.)20 μM·h (i.v.)
45 μM·h (p.o.)1.3 μM·h (i.v.)
0.2 μM·h (p.o.)- 临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点 NCT01358331 Tumor, Solid Phase 1 Terminated - - NCT03745989 Solid Tumors Phase 1 Not yet recruiting May 6, 2022 - NCT02972034 Neoplasms Col... more >>orectal Cancer Collapse << Phase 1 Recruiting October 29, 2021 United States, Michigan ... more >> Call for Information (Investigational Site 0002) Recruiting Grand Rapids, Michigan, United States, 49546 United States, Tennessee Call for Information (Investigational Site 0001) Recruiting Nashville, Tennessee, United States, 37203 Canada, Quebec Merck Canada Recruiting Kirkland, Quebec, Canada, H9H 4M7 Contact: Medical Information Centre Centre d'information medicale Merck Canada Inc. 514-428-8600 / 1-800-567-2594 Collapse << - 参考文献
- [1] Boga SB, Deng Y, et al. MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology. ACS Med Chem Lett. 2018 Jun 14;9(7):761-767.
- [2] Moschos SJ, Sullivan RJ, et al. Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors. JCI Insight. 2018 Feb 22;3(4). pii: 92352.
- [3] Roskoski R Jr, et al. Targeting ERK1/2 protein-serine/threonine kinases in human cancers. Pharmacol Res. 2019 Apr;142:151-168.
实验方案
- 计算器
- 储存液制备
技术信息
| CAS号 | 1184173-73-6 | 储存条件 |
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| 分子式 | C37H41N9O3S | 运输 | 蓝冰 | |||||
| 分子量 | 691.85 | 别名 | SCH900353 | |||||
| 溶解度 |
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动物实验配方 |
