| 產(chǎn)品描述： | LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent |
| 靶點(diǎn)： |
IC50: 38.2 nM (TGF-β receptor type 1 (ALK5));TGF-beta/Smad |
| 體內(nèi)研究： |
LY3200882 (60 mg/kg; oral gavage; twice a day; for 21 days; BALB/C female mice) treatment significantly delays tumor growth in CT26 model. LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose dependent fashion. LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer). Animal Model: BALB/C female mice (5-8-week-old) injected with CT26 cells Dosage: 60 mg/kg Administration: Oral gavage; twice a day; for 21 days Result: A statistically significant tumor growth delay in CT26 model was observed. |
| 參考文獻(xiàn)： |
1. Huaxing Pei, et al. Abstract 955: LY3200882, a novel, highly selective TGFβRI small molecule inhibitor. AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 955. 2. Xu G, et al. Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-β type 1 receptor inhibitors. Eur J Med Chem. 2020 Apr 29;198:112354. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.296 ml |
11.481 ml |
22.961 ml |
| 5 mM |
0.459 ml |
2.296 ml |
4.592 ml |
| 10 mM |
0.23 ml |
1.148 ml |
2.296 ml |
| 50 mM |
0.046 ml |
0.23 ml |
0.459 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲(chǔ)）
營業(yè)執(zhí)照(三證合一)
北京