A PI3K p110α and p110δ inhibitor
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ETP-46321

Item No. 37330

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-8-(4-morpholinyl)imidazo[1,2-a]pyrazin-6-yl]-2-pyrimidinamine
CAS Number
1252594-99-2
Molecular Formula
C20H27N9O3S
Formula Weight
473.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/ml
λmax
270 nm
SMILES
O=S(N1CCN(CC1)CC2=CN3C=C(C4=CN=C(N)N=C4)N=C(N5CCOCC5)C3=N2)(C)=O
InChi Code
InChI=1S/C20H27N9O3S/c1-33(30,31)29-4-2-26(3-5-29)12-16-13-28-14-17(15-10-22-20(21)23-11-15)25-19(18(28)24-16)27-6-8-32-9-7-27/h10-11,13-14H,2-9,12H2,1H3,(H2,21,22,23)
InChi Key
OHKDVDMWRKFZRB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    ETP-46321 is an inhibitor of PI3K p110α and p110δ (apparent Kis = 2.3 and 14.2 nM, respectively).1 It is selective for PI3K p110α and p110δ over p110β and p110γ (apparent Kis = 170 and 179 nM, respectively), as well as a panel of 288 kinases at 1 µM. ETP-46321 inhibits Akt phosphorylation in U2OS cells (IC50 = 8.3 nM). In vivo, ETP-43621 (50 mg/kg) reduces tumor volume in a K-RasG12V-driven murine lung tumor model. It also reduces anti-collagen IgG1 and IgG2a production, swelling, and joint rigidity in a mouse model of collagen-induced arthritis.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. González, S.M., Hernández, A.I., Varela, C., et al. Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. Bioorg. Med. Chem. Lett. 22(10), 3460-3466 (2012).

    2. Aragoneses-Fenoll, L., Montes-Casado, M., Ojeda, G., et al. ETP-46321, a dual p110α/δ class IA phosphoinositide 3-kinase inhibitor modulates T lymphocyte activation and collagen-induced arthritis. Biochem. Pharmacol. 106, 56-69 (2016).