TGX-221 Inhibitor CAS No. 663619-89-4

Cat. No.	Name	Size	Price
KI0010	TGX-221	5 mg	$130
	TGX-221	25 mg	$520
	TGX-221	100 mg	$1392

Chemical Characteristic

Product Name	TGX-221
CAS No.	663619-89-4
Molecular Weight	364.44
Formula	C₂₁H₂₄N₄O₂
Chemical Name	(+/-)-7-Methyl-2-(morpholin-4-yl)-9-(1-phenylaminoethyl)pyrido[1,2-a]pyrimidin-4-one
Smiles	c12nc(cc(=O)n1cc(cc2C(C)Nc1ccccc1)C)N1CCOCC1
Chemical Structure

Biological activities

TGX-221 is a potent and selective phosphoinositide 3-kinase (PI3K) p110β inhibitor with an IC50 of 8.5 nM. The IC50 value for TGX-221 against class I PI3K catalytic isoform p110α is 5 µM. In J774.2 macrophage cells, TGX-221 (50 nM) partially attenuates insulin-induced phosphorylation of Ser⁴⁷³ of protein kinase B (PKB).^[1] TGX-221 (0.1-2.5 µM) reduces the Ca²⁺ signal with about 50% in aspirin-treated, Fura-2-loaded platelets. TGX-221 also potently suppresses glycoprotein VI (GPVI)-induced InsP3 production and Akt phosphorylation in aspirin-treated human platelets. In addition, platelet treatment with PIK-75 or TGX-221, alone or in combination, suppresses convulxin- or C-reactive protein (CRP)-induced P-selectin expression with 40-50%, i.e. to the same extent as does wortmannin or LY-294002.^[2] TGX-221 (3+3 mg/kg+mg/kg/hour) significantly improves blood flow in FeCl3-induced arterial thrombosis in mice. Vascular patency (non-occluded/total arteries) is also significantly improved by treatment with the 3+3 dose of TGX-221 compared to vehicle, but there is no significant benefit with the doses of 0.3+0.3 or 1+1. Tail bleeding time in mice increases significantly in response to TGX-221 administered at the 3+3 dose (median 1560 seconds) and the 1+1 dose (median 1305 seconds) compared to vehicle (median 225 seconds). Renal bleeding time increases significantly in mice treated with all three doses of TGX-221 compared to vehicle. The plasma TGX-221 levels in mice are 0.85 µM when mice are treated with TGX-221 at a dose of 1 mg/kg and given an infusion of TGX-221 at 1 mg/kg/hour for 45 minutes.^[3]

References

[1] Chaussade C et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007, 404(3): 449-458. [2] Gilio K, et al. Non-redundant roles of phosphoinositide 3-kinase isoforms alpha and beta in glycoprotein VI-induced platelet signaling and thrombus formation. J Biol Chem. 2009, 284(49): 33750-33762 [3] Bird JE, et al. Bleeding response induced by anti-thrombotic doses of a phosphoinositide 3-kinase (PI3K)-β inhibitor in mice. Thromb Res. 2011, 127(6): 560-564.

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