Art. -Nr.: HY-103021

LY3200882

Name: LY3200882
Brand: MedChemExpress
SKU: HY-103021
Price: 110.00 USD
Availability: InStock
Rating: 5 (14 reviews)

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC₅₀ of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.

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Reinheit : 99.87%
CAS. Nr.: 1898283-02-7
Formel: C₂₄H₂₉N₅O₃
Molecular Weight:435.52

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

LY3200882 Chemical Structure

CAS. Nr.: 1898283-02-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 38.2 nM (TGF-β receptor type 1 (ALK5))^[2]

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells in a dose dependent fashion^[1].
LY3200882 shows 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^[1].
In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naive T cell activity and restore proliferation^[1].
LY3200882 inhibits NIH₃T₃ cell viability with an IC₅₀ of 82.9 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LY3200882 (60 mg/kg; oral gavage; twice a day; for 21 days; BALB/C female mice) treatment significantly delays tumor growth in CT26 model^[2].
LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose dependent fashion^[1].
LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/C female mice (5-8-week-old) injected with CT26 cells^[2]
Dosage:

60 mg/kg
Administration:

Oral gavage; twice a day; for 21 days
Result:

A statistically significant tumor growth delay in CT26 model was observed.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1898283-02-7
Appearance Solid
Molecular Weight 435.52
Formel C₂₄H₂₉N₅O₃
Color Off-white to light yellow
SMILES

OC(C)(C)C1=NC=CC(NC2=NC=CC(OC3=CN(C4CC4)N=C3C5CCOCC5)=C2)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

All Cell Proliferation/Viability AssayApoptosis AnalysisCell Migration/Invasion AssayWBHistological Imaging/Staining

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Journal Impact Factor

Nat Genet

TGF-β builds a dual immune barrier in colorectal cancer by impairing T cell recruitment and instructing immunosuppressive SPP1+ macrophages. [Abstract]

2025 Dec;57(12):3050-3065. PMID: 41203813
Sci Adv

A deubiquitination module essential for Treg fitness in the tumor microenvironment. [Abstract]

2022 Nov 25;8(47):eabo4116. PMID: 36427305
Biomaterials

The programmed site-specific delivery of LY3200882 and PD-L1 siRNA boosts immunotherapy for triple-negative breast cancer by remodeling tumor microenvironment. [Abstract]

2022 May;284:121518. PMID: 35462305
J Invest Dermatol

Identification of Small-Molecule Inhibitors Targeting Different Signaling Pathways in Cancer-Associated Fibroblast Reprogramming Under Tumor-Stroma Interaction. [Abstract]

2025 Jan;145(1):65-76.e13. PMID: 38848988
J Biol Eng

Enhancing the therapeutic efficacy of gemcitabine in bladder cancer through TGF-β1 inhibition and pluronic F-127-based microsphere delivery. [Abstract]

2025 Jul 11;19(1):62. PMID: 40646590

LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]

Bladder cancer cell lines 5637 and SW780 were treated with varying concentrations of LY3200882 (0, 1, 2.5, or 5 µM) for 48 h and assessed for cell viability using CCK8 assay.

LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]

Cells were treated with 2.5 µM LY2109761 or LY3200882 and examined for cell apoptosis by Flow cytometry.

LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]

Cell invasion capabilities using a Transwell assay treated with 2.5 µM LY2109761 or LY3200882.

LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]

The protein levels of Ki-67, Cleaved-caspase 3, E-cadherin, MMP-2, and MMP-9 using Immunoblotting treated with 2.5 µM LY2109761 or LY3200882.

LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]

Histological analysis of tumor tissues treated with LY3200882 (10 mg/kg) using H&E staining.
Mar Drugs

Anti-Inflammatory Azaphilones from the Edible Alga-Derived Fungus Penicillium sclerotiorum. [Abstract]

2021 Sep 22;19(10):529. PMID: 34677428
Bioengineering (Basel)

Proteoglycans Enhance the Therapeutic Effect of BMSC Transplantation on Osteoarthritis. [Abstract]

2024 Nov 20;11(11):1167. PMID: 39593826
FASEB J

Myeloid-specific blockade of Notch signaling alleviates murine pulmonary fibrosis through regulating monocyte-derived Ly6clo MHCIIhi alveolar macrophages recruitment and TGF-β secretion. [Abstract]

2020 Aug;34(8):11168-11184. PMID: 32638441
Cytokine

Bone marrow mesenchymal stem cells paracrine TGF-β1 to mediate the biological activity of osteoblasts in bone repair. [Abstract]

2023 Apr:164:156139. PMID: 36738525
Biol Reprod

Increased EHD1 in trophoblasts causes RSM by activating TGFβ signaling. [Abstract]

2024 Dec 12;111(6):1235-1248. PMID: 39012723
Res Sq

2025 Dec 10.
Res Sq

2025 Sep 26.
Patent

US20240238274A1.
ACS Comb Sci

Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]

2019 Dec 9;21(12):805-816. PMID: 31689077

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 33.33 mg/mL (76.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2961 mL

11.4805 mL

22.9611 mL

5 mM

0.4592 mL

2.2961 mL

4.5922 mL

10 mM

0.2296 mL

1.1481 mL

2.2961 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Huaxing Pei, et al. Abstract 955: LY3200882, a novel, highly selective TGFβRI small molecule inhibitor. AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 955.

[2]. Xu G, et al. Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-β type 1 receptor inhibitors. Eur J Med Chem. 2020 Apr 29;198:112354. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2961 mL	11.4805 mL	22.9611 mL	57.4026 mL
	5 mM	0.4592 mL	2.2961 mL	4.5922 mL	11.4805 mL
	10 mM	0.2296 mL	1.1481 mL	2.2961 mL	5.7403 mL
	15 mM	0.1531 mL	0.7654 mL	1.5307 mL	3.8268 mL
	20 mM	0.1148 mL	0.5740 mL	1.1481 mL	2.8701 mL
	25 mM	0.0918 mL	0.4592 mL	0.9184 mL	2.2961 mL
	30 mM	0.0765 mL	0.3827 mL	0.7654 mL	1.9134 mL
	40 mM	0.0574 mL	0.2870 mL	0.5740 mL	1.4351 mL
	50 mM	0.0459 mL	0.2296 mL	0.4592 mL	1.1481 mL
	60 mM	0.0383 mL	0.1913 mL	0.3827 mL	0.9567 mL

Bioz

Keywords

LY3200882

14 Cited Publications

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LY3200882

Publications Citing Use of MedChemExpress (MCE) LY3200882

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen