Cayman Chemical Item Number 10007349

(CAS 663619-89-4)

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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
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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

Pricing updated 2015-07-03. Prices are subject to change without notice.

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Cayman Chemical Company regularly evaluates our shipping methods to ensure product stability is maintained and our corporate environmental impact is minimized. Products selected for review are evaluated and shipping methods are certified by our Scientists. While occasionally our method of shipping a product may change, rest assured the shipping conditions on all Cayman Chemical products have been reviewed and validated.

Upon receipt, it is important to check the storage requirements of your products and place them at the appropriate temperature. Products shipped without ice may require frozen storage for long term stability.

Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.

Cayman Chemical

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Ann Arbor, Michigan 48108 USA


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