| 产品描述： | APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity |
| 靶点： |
Ras |
| 体外研究： |
APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay. APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-1 |
| 体内研究： |
APS6-45 (10 mg/kg; p.o. daily for 30 d) inhibits growth of TT tumors in mice and does not affect body weight. APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice. APS6-45 (20 mg/kg; a single p.o.) exhibits long half-life (5.6 h), Cmax (9.7 µM) and AUC0-24 (123.7 µM•h) in mice. Animal Model: Female nude mice (6 weeks) are implanted with TT cells Dosage: 10 mg/kg Administration: P.o. daily for 30 days Result: Led to partial or complete responses in 75% and was well tolerated. Animal Model: Male ICR mice (6 weeks of age) Dosage: 20 mg/kg (Pharmacokinetic Analysis) Administration: A single p.o. Result: T1/2=5.6 h, Cmax=9.7 µM, AUC0-24=123.7 µM•h. |
| 参考文献： |
1. Sonoshita M, et, al. A whole-animal platform to advance a clinical kinase inhibitor into new disease space. Nat Chem Biol. 2018 Mar;14(3):291-298. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.824 ml |
9.118 ml |
18.235 ml |
| 5 mM |
0.365 ml |
1.824 ml |
3.647 ml |
| 10 mM |
0.182 ml |
0.912 ml |
1.824 ml |
| 50 mM |
0.036 ml |
0.182 ml |
0.365 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京