貨號	規格	價格	上海	北京	武漢	南京
S88531-2mg	99.8%	￥200.00 S88531-2mg ￥200.00 現貨	4 4	-	-	-
S88531-5mg	99.8%	￥320.00 S88531-5mg ￥320.00 現貨	5 5	-	-	-
S88531-10mg	99.8%	￥490.00 S88531-10mg ￥490.00 現貨	6 6	-	-	-
S88531-25mg	99.8%	￥830.00 S88531-25mg ￥830.00 現貨	6 6	-	-	-
S88531-50mg	≥98%	￥1250.00 S88531-50mg ￥1250.00 2-3天	0 貨期：2-3天	-	-	-
S88531-100mg	≥98%	￥1750.00 S88531-100mg ￥1750.00 2-3天	0 貨期：2-3天	-	-	-

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產品介紹

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

產品描述：

靶點：

IC50: 38.2 nM (TGF-β receptor type 1 (ALK5));TGF-beta/Smad

體內研究：

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：

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：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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LY-3200882

2-(4-((4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)oxy)pyridin-2-yl)amino)pyridin-2-yl)propan-2-ol