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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
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