LY3200882 是一种高度选择性的、口服活性的、具有 ATP 竞争性的 TGF-β 受体 1 型 (ALK5) 抑制剂(IC50:38.2 nM)。它能够抑制多种促肿瘤活性，可用作免疫调节剂。

LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).

LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells. LY3200882 has shown anti-metastatic activity in vitro in migration assays. In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed na?ve T cell activity and restore proliferation [1].

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) [1].

1898283-02-7

C24H29N5O3

435.528

DMSO:85 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years