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Background Information:
LY3200882 is a next generation small molecule inhibitor of TGF-β receptor type 1 (TGFβRI) and a promising immune modulatory agent. It is a potent, highly selective inhibitor of TGFβRI embodied in a structural platform with a synthetically scalable route, in an ATP competitive fashion to the serine-threonine kinase domain of TGFβRI. Mechanism of action studies reveal that LY3200882 inhibits various pro-tumorigenic activities. 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. 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. 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 also showed anti-metastatic activity in vitro in migration assays as well as in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer). Finally, LY3200882 shows combinatorial anti-tumor benefits with checkpoint inhibition (anti-PD-L1) in the syngeneic CT26 model (ref. 1).
Reference:
1. H. Pei, et al, LY3200882, a novel, highly selective TGFβRI small molecule inhibitor [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 955. doi:10.1158/1538-7445.AM2017-955.
APIM050191: LY-3200882 (LY3200882)
CAS No.: 1898283-02-7.
Molecular Formula: C24H29N5O3.
Molecular Weight: 435.5.
Purity: >99.5% by HPLC at 214 and 254 nm.
QC: HPLC-MS, H-NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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