 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 663619-89-4 |
| Molecular formula(MF) | C21H24N4O2 |
| Molecular Weight(MW): | 364.44 |
| Alias | (+/-)-7-Methyl-2-(morpholin-4-yl)-9-(1-phenylaminoethyl)pyrido[1,2-a]pyrimidin-4-one |
| In vitro | DMSO | 12 mg/mL (32.92 mM) |
|---|---|---|
| Water | <1 mg/mL | |
| Ethanol | <1 mg/mL | |
| In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 30 mg/mL |
| Description | TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α. | |||||||||||||||||||||||||||||||||||||
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| Targets |
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| In vitro |
The activity of TGX-221 against different isoforms is measured in an in vitro PI3K assay using multiple preparations of recombinant p85/p110. TGX-221 show slow potent to p110δ with IC50 of 211 nM. Furthermore, TGX-221 partially attenuates insulin-induced phosphorylation of Ser473 of PKB in J774.2 macrophage cells. [1] TGX-221 inhibits platelet-ECC interaction, platelet aggregation and platelet-granulocyte binding in an extracorporeal circulation (ECC) model. [2] A recent study shows that after treatment with TGX-221 (0.2, 2, and 20 μM), PC3 cells show inhibition of proliferation with a significant reduction of the activity of the p110β PI3K isoform. [3] |
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| Cell Data |
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| In vivo | As an anti-thrombotic agent, TGX-221 at doses 1 + 1 (49 %) and 3+3 (88 %) improves integrated blood flow over 30 minutes in a mouse model. In addition, Tail bleeding time (BT) (sec) increases with TGX-221 doses of 3 + 3 (median 1560) and 1 + 1 (1305) and mean renal BT (sec) also increases in all TGX-221 groups. [4] |