LY3200882

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[1][2].

Product Specifications

CAS Number

[1898283-02-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

TGF-β Receptor

Type

Reference compound

Related Pathways

TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/LY3200882.html

Purity

99.87

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C24H29N5O3

Molecular Weight

435.52

Precautions

H302, H315, H319, H335

References & Citations

[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.