InformationLY 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.TargetsTGFβRIIn vitroLY3200882 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 vivoIn 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. Specification: 0.99 Molecular Formula: C24H29N5O3 Molecular Weight: 435.52 PubChem CID: 121249291 Isomeric SMILES: CC(C)(C1=NC=CC(=C1)NC2=NC=CC(=C2)OC3=CN(N=C3C4CCOCC4)C5CC5)O Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/L414169-SCI_95d359c0d20dcb07088d5e5bd1046e01.pdf
- UPC:
- 51112514
- Condition:
- New
- Availability:
- 2 weeks
- Weight:
- 0.96 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- L414169-5mg
- CAS:
- 1898283-02-7
- Product Size:
- 5mg
- Hazard Statement Codes:
- H302:H315:H319:H335
- Precautionary Statement Codes:
- P261:P305+P351+P338
