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首页-小分子抑制剂&激动剂-TGF-beta/Smad-TGF beta Receptor (TGFBR)-LY2109761
LY2109761

Chemical Structure : LY2109761

CAS No.: 700874-71-1

LY2109761 (LY 2109761;LY-2109761)

货号: PC-42887Not For Human Use, Lab Use Only.

LY2109761 is a potent, selective and orally active TGF-β RI/II dual inhibitor with Ki of 38/300 nM, respectively.

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25 mg ¥1480 In stock
50 mg ¥2380 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LY2109761 is a potent, selective and orally active TGF-β RI/II dual inhibitor with Ki of 38/300 nM, respectively.
LY2109761 completely inhibits TGF-β-induced Sma2 phosphorylation on tumor cells or the liver microenviroment, inhibits the L3.6pl/GLT soft agar growth。
LY2109761 suppresses both basal and TGF-β1-induced cell migration and invasion, and stimulates anoikis in vitro。
LY2109761 significantly reduces the tumor burden as well as spontaneous abdominal metastases, and prolongs survival combined with gemicitabine in vivo model of pancreatic cancer.

物理化学性质&存储条件

分子量 441.5249
分子式 C26H27N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Quinoline, 4-[5,6-dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]-

参考文献

1. Mazzocca A, et al. Hepatology. 2009 Oct;50(4):1140-51.

2. Zhang M, et al. Cancer Res, 2011, 71(23), 7155-7167.

3. Melisi D, et al. Mol Cancer Ther, 2008, 7(4), 829-840.

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