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TGX 221

Cat. No. 5832 Submit a Review Datasheet / COA / SDS
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Description: Potent and selective PI 3-kinase β inhibitor
Chemical Name: 7-Methyl-2-(4-morpholinyl)-9-[1-(phenylamino)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one
Purity: ≥98% (HPLC)
Datasheet
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for TGX 221

TGX 221 is a potent and selective PI 3-kinase β inhibitor (IC50 values are 0.007, 0.1, 3.5 and 5 μM for the β, δ, γ and α isoforms, respectively). Shows >1,000-fold selectively for PI 3-kinase β over a range of other kinases. Inhibits thrombus formation in animal models.

Compound Libraries for TGX 221

TGX 221 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for TGX 221

M. Wt 364.44
Formula C21H24N4O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 663619-89-4
PubChem ID 9907093
InChI Key CPRAGQJXBLMUEL-UHFFFAOYSA-N
Smiles CC(C1=CC(C)=CN2C(C=C(N3CCOCC3)N=C12)=O)NC4=CC=CC=C4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for TGX 221

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 18.22 50

Preparing Stock Solutions for TGX 221

The following data is based on the product molecular weight 364.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 5.49 mL 27.44 mL 54.88 mL
2.5 mM 1.1 mL 5.49 mL 10.98 mL
5 mM 0.55 mL 2.74 mL 5.49 mL
25 mM 0.11 mL 0.55 mL 1.1 mL

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References for TGX 221

References are publications that support the biological activity of the product.

Condliffe et al (2005) Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils. Blood 106 1432 PMID: 15878979

Jackson et al (2005) PI 3-kinase p110β: a new target for antithrombotic therapy. Nat.Med. 11 507 PMID: 15834429

If you know of a relevant reference for TGX 221, please let us know.

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Citations for TGX 221

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