An inhibitor of PI3K
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GNE-490

Item No. 41120

Technical Information
Formal Name
2-(2-amino-4-methyl-5-pyrimidinyl)-α,α-dimethyl-4-(4-morpholinyl)-thieno[3,2-d]pyrimidine-6-methanol
CAS Number
1033739-92-2
Molecular Formula
C18H22N6O2S
Formula Weight
Purity
≥98%
A solid
DMSO: Soluble: ≥10 mg/ml
SMILES
OC(C)(C)C1=CC(N=C(C2=CN=C(N)N=C2C)N=C3N4CCOCC4)=C3S1
InChi Code
InChI=1S/C18H22N6O2S/c1-10-11(9-20-17(19)21-10)15-22-12-8-13(18(2,3)25)27-14(12)16(23-15)24-4-6-26-7-5-24/h8-9,25H,4-7H2,1-3H3,(H2,19,20,21)
InChi Key
SFWTVVNNVHWDEE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GNE-490 is an inhibitor of PI3K (IC50s = 3.5, 25, 5.2, and 15 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively).1 It is selective for PI3K over mTOR (IC50 = 740 nM) and a panel of 142 kinases at 1 µM. GNE-490 (0.4 µM) reduces cell migration by, the number of vessel outgrowths from, and induces apoptosis in, human umbilical vein endothelial cells (HUVECs).2 It increases the length of circadian rhythms in zebrafish larvae.3 GNE-490 (30 mg/kg) decreases vascularization and tumor growth in a PC3 prostate cancer mouse xenograft model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sutherlin, D.P., Sampath, D., Berry, M., et alDiscovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors. J. Med. Chem. 53(3), 1086-1097 (2010).

    2. Sampath, D., Oeh, J., Wyatt, S.K., et alMultimodal microvascular imaging reveals that selective inhibition of class I PI3K is sufficient to induce an antivascular response. Neoplasia 15(7), 694-711 (2013).

    3. Mosser, E.A., Chiu, C.N., Tamai, T.K., et alIdentification of pathways that regulate circadian rhythms using a larval zebrafish small molecule screen. Sci. Rep. 9(1), 12405 (2019).