aladdin 阿拉丁 L414169 LY 3200882 1898283-02-7 99%

中文名：LY 3200882

英文名：LY 3200882

英文别名：LY3200882|1898283-02-7|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|19HY34R6UN|LY 3200882|2-[4-[[4-[1-Cyclopropyl-3-(oxan-4-yl)pyrazol-4-yl]oxypyridin-2-yl]amino]pyridin-2

纯度：99%

货号：L414169

包装：5mg、100mg、10mg

Cas号：1898283-02-7

存储温度：-20°C储存

产品介绍：

Information

LY 3200882 is a potent, highly selective inhibitor ofTGF-β receptor type 1 (TGFβRI). It potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion.

Targets

TGFβRI

In vitro

LY3200882 inhibits various pro-tumorigenic activities. LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion. In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naïve T cell activity and restore proliferation. It acts as an immune modulatory agent.

In vivo

In preclinical tumor models, LY3200882 showed potent anti-tumor activity in the orthotopic 4T1-LP model of triple negative breast cancer and this activity correlated with enhanced tumor infiltrating lymphocytes in the tumor microenvironment. Durable tumor regressions in the orthotopic 4T1-LP model were observed and rechallenge of congenic tumors resulted in complete rejection in all mice. LY3200882 has shown anti-metastatic activity in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer). In addition, LY3200882 shows combinatorial anti-tumor benefits with checkpoint inhibition (anti-PD-L1) in the syngeneic CT26 model.

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