TGX-221

Cayman Chemical Item Number 10007349

(CAS 663619-89-4)

TGX-221 (CAS 663619-89-4)

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Description

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).1,2,3 Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are 4 isoforms (p110α, p110β, p110δ, and p100γ), and a p85 regulatory subunit.3 TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.4 Inhibition appears to occur at the ATP binding site based on the observed increase in IC50 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 of 50 nM.4 Selective inhibition of PI3K p110β results in defective platelet thrombus formation and defines PI3K as a target for antithrombotic therapy.4

1 Rameh, L.E., and Cantley, L.C. The role of phosphoinositide 3-kinase lipid products in cell function. J Biol Chem 274 8347-8350 (1999).

2 Vivanco, I., and Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nat Rev Cancer 2 489-501 (2002).

3 Hennessy, B.T., Smith, D.L., Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nat Rev Drug Discov 4 988-1004 (2005).

4 Jackson, S.P., Schoenwaelder, S.M., Goncalves, I., et al. PI 3-kinase p110b: A new target for antithrombotic therapy. Nat Med 11(5) 507-514 (2005).

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
Formulation A solution in ethanol
Purity >98%
λmax 268 nm
Stability 1 year
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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Cc1cc(C(C)​Nc2ccccc2)​c2nc(cc(=O)​n2c1)​N1CCOCC1
InCHI Code
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​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
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CPRAGQJXBLMUEL-UHFFFAOYSA-N

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TGX-221 is available in the following screening library:

Size Price Quantity Subtotal
500 µg $49.00 $0.00
1 mg $69.00 $0.00
5 mg $98.00 $0.00
10 mg $176.00 $0.00
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Cart Total $0.00

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Pricing updated 2014-04-16. Prices are subject to change without notice.

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