TGX-221 | Potent and selective PI3Kß inhibitor

CAS:
 663619-89-4
Catalog Number:
 10-4783

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5 mg$55.00
25 mg$195.00

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
CAS:
663619-89-4
Catalog Number:
10-4783
Activity:
Potent and selective PI3-Kß inhibitor
Chemical Names:
9-(1-Anilinoethyl)-7-methyl-2-morpholino-4-ylpyrido[1,2-a]pyrimidin-4-one
Alternate Name:
7-Methyl-2-morpholino-9-(1-(phenylamino)ethyl)-4H-pyrido[1,2-a]pyrimidin-4-one
Molecular Weight:
364.45
Molecular Formula:

C21H24N4O2

Solubility:
Soluble in DMSO (10 mg/mL)
Physical Properties:
Off-white solid
Purity:

98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO or water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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