TGX 221

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Cat.No. 5832 - TGX 221 | C21H24N4O2 | CAS No. 663619-89-4
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
Citations
Reviews
Literature

Biological Activity

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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

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

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

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


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Keywords: TGX 221, TGX 221 supplier, TGX221, PI3K, PI, 3-kinase, phosphoinositide, potent, selective, inhibits, inhibitors, beta, β, antithrombotic, 3-Kinase, 5832, Tocris Bioscience

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