Home TGF-beta/Smad TGF-beta/Smad inhibitor LY 3200882 For research use only.

LY 3200882

LY 3200882 is a potent, highly selective inhibitor of TGF-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.

LY 3200882 Chemical Structure

LY 3200882 Chemical Structure

CAS No. 1898283-02-7

Purity & Quality Control

Batch: S877201 DMSO]87 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.93%
99.93

LY 3200882 Related Products

Signaling Pathway

TGF-beta/Smad Signaling Pathways

TGF-beta/Smad Signaling Pathway

Biological Activity

Description LY 3200882 is a potent, highly selective inhibitor of TGF-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 [1]
In vitro
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[1].
In Vivo
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[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04031872 Unknown status
Colorectal Cancer Metastatic
The Netherlands Cancer Institute|Vall d''Hebron Institute of Oncology|Agendia|European Organisation for Research and Treatment of Cancer - EORTC|Azienda Ospedaliera Niguarda Cà Granda|Fundación para la Investigación del Hospital Clínico de Valencia|University of Campania Luigi Vanvitelli|University of Turin Italy|Eli Lilly and Company|Catalan Institute of Health|Universitaire Ziekenhuizen KU Leuven
 February 2020 Phase 1|Phase 2
NCT04158700 Withdrawn
Advanced Cancer
Eli Lilly and Company|Merck Sharp & Dohme LLC
 December 5 2019 Phase 1|Phase 2
NCT03792139 Completed
Healthy
Eli Lilly and Company
 January 8 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 435.52 Formula

C24H29N5O3
CAS No. 1898283-02-7 SDF --
Smiles CC(C)(C1=NC=CC(=C1)NC2=NC=CC(=C2)OC3=CN(N=C3C4CCOCC4)C5CC5)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 87 mg/mL ( (199.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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