A pan inhibitor of class I PI3K isoforms
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GDC-0941

Item No. 11600

Technical Information
Formal Name
2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-thieno[3,2-d]pyrimidine
CAS Number
957054-30-7
Synonyms
  • GNE-0941
  • Pictilisib
  • Pictrelisib
Molecular Formula
C23H27N7O3S2
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS (pH 7.2) (1:5): 0.15 mg/ml
λmax
213, 260, 319 nm
SMILES
CS(N(CC1)CCN1CC(S2)=CC3=C2C(N4CCOCC4)=NC(C5=C(C=NN6)C6=CC=C5)=N3)(=O)=O
InChi Code
InChI=1S/C23H27N7O3S2/c1-35(31,32)30-7-5-28(6-8-30)15-16-13-20-21(34-16)23(29-9-11-33-12-10-29)26-22(25-20)17-3-2-4-19-18(17)14-24-27-19/h2-4,13-14H,5-12,15H2,1H3,(H,24,27)
InChi Key
LHNIIDJUOCFXAP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival.1,2 GDC-0941 is a potent pan inhibitor of class I catalytic subunits of PI3K, inhibiting p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively.3,4 It is much less effective against class II-IV isoforms of PI3K and against mTOR.3,5 GDC-0941 inhibits the growth of certain types of cancer cells and blocks signaling through PI3K to Akt, both in cells and in vivo.3,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hennessy, B.T., Smith, D.L., Ram, P.T., et alExploiting the PI3K/AKT pathway for cancer drug discovery. Nat. Rev. Drug Discov. 4(12), 988-1004 (2005).

    2. Hirsch, E., Ciraolo, E., Ghigo, A., et alTaming the PI3K team to hold inflammation and cancer at bay. Pharmacol. Ther. 118(2), 192-205 (2008).

    3. Folkes, A.J., Ahmadi, K., Alderton, W.K., et alThe identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. J. Med. Chem. 51(18), 5522-5532 (2008).

    4. Berndt, A., Miller, S., Williams, O., et alThe p110δ structure: Mechanisms for selectivity and potency of new PI(3)K inhibitors. Nat. Chem. Biol. 6(2), 117-124 (2010).

    5. 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).

    6. Raynaud, F.I., Eccles, S.A., Patel, S., et alBiological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: From PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Mol. Cancer Ther. 8(7), 1725-1738 (2009).