TGX-221 | Potent and selective PI3Kß inhibitor

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5 mg$55.00
25 mg$195.00
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Highly-Selective Kinase Inhibitor Library PI3K Inhibitors

TGX-221 (663619-89-4) 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

References/Citations:

  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
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Alternate Name:
7-Methyl-2-morpholino-9-(1-(phenylamino)ethyl)-4H-pyrido[1,2-a]pyrimidin-4-one

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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

TGX-221 (663619-89-4) 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

References/Citations:

  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