TGX-221
Potent and selective PI3Kß inhibitor / TGX-221 is a potent (IC50 = 5 nM) and selective (1000-fold over p110α and p110γ) inhibitor of PI3-kinase isoform p110ß.1 Displays anti-thrombotic activity without affecting bleeding time.1,2 It significantly inhibited tumorigenesis in VHL, SETD2, PTEN, and CDKN2A mutated clear cell renal cell carcinoma.3 TGX-221 induced apoptosis in glioblastoma cells and inhibited cell migration and invasion.4
Biochemicals & reagents
663619-89-4
7-Methyl-2-morpholino-9-(1-(phenylamino)ethyl)-4H-pyrido[1,2-a]pyrimidin-4-one
1) Jackson et al. (2005), PI 3-kinase p110ß: a new target for antithrombotic therapy; Nat. Med. 11 507 2) Sturgeon et al. (2008), Advantages of a selective beta-isoform phosphoinositide 3-kinase antagonist, an anti-thrombotic agent devoid of other cardiovascular actions in the rat; Nature 587 209 3) Feng et al. (2015), PI3Kß Inhibitor TGX221 Selectively Inhibits Renal Cell Carcinoma Cells with Both VHL and SETD2 Mutations and Links Multiple Pathways; Sci. Rep. 5 9465 4) Yang et al. (2017), TGX-221 inhibits proliferation and induces apoptosis in human glioblastoma cells; Oncol. Rep. 38 2836
-20°C
TARGET: Kinase -- PATHWAY: Coagulation; PI3K -- DISEASE AREA: Cancer