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TGX-221

Supplier:
Catalogue number:
10-4783-01
Size:
5 mg
Product is available in:
  • USA
  • Canada
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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

Product Type:

Biochemicals & reagents

CAS Number:

663619-89-4

Alternative Names:

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

Reference:

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

Storage Temperature:

-20°C

Additional Information:

TARGET: Kinase -- PATHWAY: Coagulation; PI3K -- DISEASE AREA: Cancer