TGX-221

SKU: orb1305205

Description

TGX-221 is a potent, selective, and cell-permeable inhibitor targeting the PI3K p110β isoform. It is widely used in cancer research to investigate PI3Kβ signaling in both cellular assays and animal models, particularly for studying tumor progression and therapeutic resistance.

Research Area

Signal Transduction

Key Properties

• CAS Number: 663619-89-4
• MW: 364.5
• Purity: >98%
• Formula: C₂₁H₂₄N₄O₂
• SMILES: CC(Nc1ccccc1)c1cc(C)cn2c1nc(cc2=O)N1CCOCC1
• Target: Kinase
• Solubility: Soluble in DMSO (up to at least 10 mg/ml)

Bioactivity

• Target IC50:
  p110β:5 nM|p110δ:0.1 μM
• In Vivo:
  In J774.2 macrophages, TGX-221 inhibits the phosphorylation of Ser473 on PKB induced by insulin. It also impedes platelet-ECC (extracorporeal circulation) interactions, platelet aggregation, and the binding between platelets and granulocytes in an ECC model. Furthermore, in the PC3 cells, TGX-221 (at concentrations of 0.2-20 μM) can suppress cell proliferation and reduce the activity of the p110β subunit of PI3K.
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• In Vitro:
  In mouse models, TGX-221 has been shown to enhance blood flow, prolonging tail bleeding and renal bleeding time.
• Cell Research:
  For measurement of proliferation, cells are seeded in triplicate in 96-well culture plates and incubated overnight to allow cell attachment. The cells are incubated with TGX-221 for 24, 48, and 72 hours. At designated time intervals, cells are quantified by a crystal violet staining-based colorimetric assay. Briefly, cells are fixed by addition of 100 μl of 2.5% glutaraldehyde solution and incubated at room temperature for 30 minutes. Plates are washed three times by submersion in PBS solution. Plates are air-dried and stained by addition of 100 μL of 0.1% solution of crystal violet dissolved in deionized water and incubated for 20 minutes at room temperature, excess dye is removed by extensive washing with deionized water, and plates are air-dried prior to bound dye solubilization in 100 μL of 10% acetic acid. The optical density of dye extracts is measured directly in plates using a microplate reader at 570 nm.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

9907093