TGX-221

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol-3,4-bisphosphate (PtdIns-(3,4)-P2) and PtdIns-(3,4,5)-P3. Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are 4 isoforms (p110alpha, p110beta, p110delta, and p100gamma), and a p85 regulatory subunit. TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110beta. Inhibition appears to occur at the ATP binding site based on the observed increase in IC50 value from 5 to ~50 nM at ATP concentrations of 50 µM and 1 mM, respectively. TGX-221 inhibits PtdIns-(3,4)-P2 production in platelets with an IC50 value of 50 nM. Selective inhibition of PI3K p110beta results in defective platelet thrombus formation and defines PI3K as a target for antithrombotic therapy.Formal Name: 7-methyl-2-(4-morpholinyl)-9-[1-(phenylamino)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one. CAS Number: 663619-89-4. Molecular Formula: C21H24N4O2. Formula Weight: 364.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 50 mg/ml, Ethanol:PBS (pH 7.2)(1:8): 0.5 mg/ml. lambdamax: 268 nm. SMILES: CC(C=C1C(NC2=CC=CC=C2)C)=CN3C1=NC(N4CCOCC4)=CC3=O. InChi Code: InChI=1S/C21H24N4O2/c1-15-12-18(16(2)22-17-6-4-3-5-7-17)21-23-19(13-20(26)25(21)14-15)24-8-10-27-11-9-24/h3-7,12-14,16,22H,8-11H2,1-2H3. InChi Key: CPRAGQJXBLMUEL-UHFFFAOYSA-N.