A dual inhibitor of PI3K and mTOR
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GDC-0980

Item No. 18303

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S)-1-[4-[[2-(2-amino-5-pyrimidinyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-2-hydroxy-1-propanone
CAS Number
1032754-93-0
Synonyms
  • Apitolisib
  • RG7422
Molecular Formula
C23H30N8O3S
Formula Weight
498.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS (pH 7.2)(1:5): 0.15 mg/ml
λmax
205, 271 nm
SMILES
O=C([C@@H](O)C)N(CC1)CCN1CC(S2)=C(C)C3=C2C(N4CCOCC4)=NC(C5=CN=C(N)N=C5)=N3
InChi Code
InChI=1S/C23H30N8O3S/c1-14-17(13-29-3-5-31(6-4-29)22(33)15(2)32)35-19-18(14)27-20(16-11-25-23(24)26-12-16)28-21(19)30-7-9-34-10-8-30/h11-12,15,32H,3-10,13H2,1-2H3,(H2,24,25,26)/t15-/m0/s1
InChi Key
YOVVNQKCSKSHKT-HNNXBMFYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $198

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    10 mg

    $329

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    25 mg

    $655

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    Product Description

    GDC-0980 is a potent inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms, with IC50 values of 5, 27, 7, and 14 nM for PI3Kα, β, δ, and γ, respectively, in cell-free assays.1,2 It also inhibits mTOR (Ki = 17 nM) but is inactive against a large panel of additional kinases.1,2 GDC-0980 induces cell cycle arrest or apoptosis in a range of cancer cell lines.2 It is effective in vivo, suppressing the growth of a number of tumor xenografts in mice and enhancing the antitumor activity of docetaxel (Item No. 11637) in mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sutherlin, D.P., Bao, L., Berry, M., et al. Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. J. Med. Chem. 54(21), 7579-7587 (2011).

    2. Wallin, J.J., Edgar, K.A., Guan, J., et al. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol. Cancer Ther. 10(12), 2426-2436 (2011).