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LY 3200882 TGF-beta/Smad inhibitor

Name: LY 3200882
Brand: Selleck Chemicals
SKU: S8772
Rating: 5 (5 reviews)

Cat.No.S8772

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 tumour and immune cells and in vivo in subcutaneous tumours in a dose dependent fashion.

Chemical Structure

Molecular Weight: 435.52

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.93

Related Targets	PKC ROCK Bcr-Abl
Other TGF-beta/Smad Inhibitors	SB431542 RepSox (E-616452) Vactosertib (TEW-7197) LDN-193189 A-83-01 LDN-193189 Dihydrochloride Galunisertib (LY2157299) SRI-011381 (C381) LY2109761 SIS3 Hydrochloride

Chemical Information, Storage & Stability

Molecular Weight	435.52	Formula	C₂₄H₂₉N₅O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1898283-02-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)(C1=NC=CC(=C1)NC2=NC=CC(=C2)OC3=CN(N=C3C4CCOCC4)C5CC5)O

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (199.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.350mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 87 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.087mg/ml (2.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 21.74 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	TGFβRI
In vitro	LY3200882 inhibits various pro-tumourigenic activities. LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumour and immune cells and in vivo in subcutaneous tumours 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 tumour models, LY3200882 showed potent anti-tumour activity in the orthotopic 4T1-LP model of triple negative breast cancer and this activity correlated with enhanced tumour infiltrating lymphocytes in the tumour microenvironment. Durable tumour regressions in the orthotopic 4T1-LP model were observed and rechallenge of congenic tumours resulted in complete rejection in all mice. LY3200882 has shown anti-metastatic activity in an experimental metastasis tumour model (intravenous EMT6-LM2 model of triple negative breast cancer). In addition, LY3200882 shows combinatorial anti-tumour benefits with checkpoint inhibition (anti-PD-L1) in the syngeneic CT26 model.
References	[1] http://cancerres.aacrjournals.org/content/77/13_Supplement/955

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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