A potent, selective PI3K inhibitor
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TGX-221

Item No. 10007349

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 50 mg/mlEthanol:PBS (pH 7.2)(1:8): 0.5 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $36

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    1 mg

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    5 mg

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    10 mg

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    Product Description

    TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.1 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.1 Selective inhibition of PI3K p110β results in defective platelet thrombus formation and defines PI3K as a target for antithrombotic therapy.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jackson, S.P., Schoenwaelder, S.M., Goncalves, I., et al. PI 3-kinase p110ß: A new target for antithrombotic therapy. Nat. Med. 11(5), 507-514 (2005).

    Product Citations

    Small, J.C., Joblin-Mills, A., Carbone, K., et al. Phenotypic screening for small molecules that protect b-cells from glucolipotoxicity. ACS Chem. Biol. 17(5), 1131-1142 (2022).