Apitolisib (GDC-0980, RG7422)

製品コードS2696 別名:GNE 390

Apitolisib (GDC-0980, RG7422)化学構造


Apitolisib (GDC-0980, RG7422)は一種の有効なI型PI3K阻害剤で、無細胞試験でPI3Kα/β/δ/γに作用する時のIC50値が5 nM/27 nM/7 nM/14 nMそれぞれ分かれます。Apitolisib (GDC-0980, RG7422)も一種のmTOR阻害剤で、無細胞試験でKi値が17 nMになって、他のPIKK家族キナーゼに作用する選択性より高くなります。臨床2期。

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  • Immunoblots from AR + TNBC cell lines treated with either CDX (25 uM), GDC-0941 (300 nM) or GDC0980 (100 nM) as single agents or CDX in combination with either GDC-0941 or GDC-0980 for 48 h analyzed for AR, p-AKT, AKT, p-S6, S6 and glyceraldehyde-3-phosphate dehydrogenase (GAPDH) protein.

    Breast Cancer Res 2014 16(4), 406. Apitolisib (GDC-0980, RG7422) purchased from Selleck.

    H2596 (B) and H513 (C) cells, were treated with ARQ 197, GDC-0980, NVP-BEZ235 alone and in combination for 48 h. Cell lysates were prepared and immunoblotted for total PARP, cleaved PARP, cyclin D1 and actin as a loading control. H2596 cells treated with ARQ 197, GDC-0980, NVP-BEZ235 alone and in combination for 48 h, the cells were then stained with Annexin V-FITC/PI and analyzed by flow cytometry.

    PLoS One 2014 9(9), e105919. Apitolisib (GDC-0980, RG7422) purchased from Selleck.

  • PI3K/mTOR inhibitor GDC-0980 supresses cell growth of A549 by inhibiting Akt/mTOR signaling pathway.  A. A549 cells were incubated for 72 hours with various concentrations of GDC-0980. Cell growth was determined by MTT assay.  B. A549 cells were incubated with GDC-0980 for 1 hour. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.

    Dr.Wang Wei from NanFang Hospital. Apitolisib (GDC-0980, RG7422) purchased from Selleck.

    After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of GDC-0980 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

    Dr. Zhang of Tianjin Medical University. Apitolisib (GDC-0980, RG7422) purchased from Selleck.




製品説明 Apitolisib (GDC-0980, RG7422)は一種の有効なI型PI3K阻害剤で、無細胞試験でPI3Kα/β/δ/γに作用する時のIC50値が5 nM/27 nM/7 nM/14 nMそれぞれ分かれます。Apitolisib (GDC-0980, RG7422)も一種のmTOR阻害剤で、無細胞試験でKi値が17 nMになって、他のPIKK家族キナーゼに作用する選択性より高くなります。臨床2期。
特性 A potent, selective, and orally available inhibitor of PI3Kα, β, δ, γ and mTOR.
p110α [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
mTOR [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
5 nM 7 nM 14 nM 17 nM(Ki app) 27 nM
In vitro試験

GDC-0980 shows the potent and selective inhibitory activities against class I PI3K and mTOR kinase versus a large panel of kinases with Ki of 17 nM for mTOR and IC50 of 5 nM, 27 nM, 7 nM, and 14 nM for PI3Kα, β, δ, and γ, respectively. [1] In vitro, GDC-0980 significantly inhibits cell proliferation in PC3 and MCF7 cells with IC50 of 307 nM and 255 nM, respectively. [1] A recent study shows that GDC-0980 reduces cancer cell viability by inhibiting cell-cycle procession and inducing apoptosis with most potency in prostate (IC50 < 200 nM 50%), <500 nM 100%), breast (IC50 <200 nM 37%, <500 nM 78%) and NSCLC lines (IC50 <200 nM 29%, <500 nM 88%) and less potency in pancreatic (IC50 <200 nM 13%, <500 nM 67%) and melanoma cell lines (IC50 <200 nM 0%, <500 nM 33%). [2]

In vivo試験 In both PC-3 and MCF-7 neo/HER2 xenograft models, GDC-0980 at a dose of 1 mg/kg, exhibits significant antitumor activity by causing tumor growth delay. Furthermore, GDC-0980 results in tumor stasis or regressions at the maximum tolerated dose of 7.5 mg/kg. [1] In mice, intravenous GDC-0980 administration at 1 mg/kg leads to low clearance (Clp: 9.2 mL/min/kg, Vss: 1.7 L/kg). While, oral administration at 5 mg/kg in 80% PEG400 and at 50 mg/kg as a crystalline suspension in 0.5% methylcellulose/0.2% Tween-80 also results in favorable pharmacokinetic parameters. [1]


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Enzymatic activity:

Enzymatic activity of the Class I PI3K isoforms is measured using a fluorescence polarization assay that monitors formation of the product 3,4,5-inositoltriphosphate molecule as it competes with fluorescently labeled PIP3 for binding to the GRP-1 pleckstrin homology domain protein. An increase in phosphatidyl inositide-3-phosphate product results in a decrease in fluorescence polarization signal as the labeled fluorophore is displaced from the GRP-1 protein binding site. Class I PI3K isoforms are expressed and purified as heterodimeric recombinant proteins. PI3K isoforms are assayed under initial rate conditions in the presence of 10 mM Tris (pH 7.5), 25 μM ATP, 9.75 μM PIP2, 5% glycerol, 4 mM MgCl2, 50 mM NaCl, 0.05% (v/v) Chaps, 1 mM dithiothreitol, 2% (v/v) DMSO at the following concentrations for each isoform: PI3Kα,β at 60 ng/mL; PI3Kγ at 8 ng/mL; PI3Kδ at 45 ng/mL. After assay for 30 minutes at 25°C, reactions are terminated with a final concentration of 9 mM EDTA, 4.5 nM TAMRA-PIP3, and 4.2 μg/mL GRP-1 detector protein before reading fluorescence polarization on an Envision plate reader. IC50s are calculated from the fit of the dose−response curves to a 4-parameter equation.Human recombinant mTOR(1360−2549) is expressed and purified from insect cells and assayed using a Lanthascreen fluorescence resonance energy transfer format in which phosphorylation of recombinant green fluorescent protein (GFP)-4-EBP1 is detected using a terbium-labeled antibody to phospho-threonine 37/46 of 4-EBP1. Reactions are initiated with ATP and conducted in the presence of 50 mM Hepes (pH 7.5), 0.25 nM mTOR, 400 nM GFP-4E-BP1, 8 μM ATP, 0.01% (v/v) Tween 20, 10 mM MnCl2, 1 mM EGTA, 1 mM dithiothreitol, and 1% (v/v) DMSO. Assays are conducted under initial rate conditions at room temperature for 30 minutes before terminating the reaction and detecting product in the presence of 2 nM Tb-anti-p4E-BP1 antibody and 10 mM EDTA. Dose−response curves are fit to an equation for competitive tight-binding inhibition and apparent Ki' s are calculated using the determined Km for ATP of 6.1 μM.
細胞アッセイ: [1]
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  • 細胞株: PC3 and MCF7.1
  • 濃度: 0 to 10 μM
  • 反応時間: 72 hours or 96 hours
  • 実験の流れ: Antiproliferative cellular assays are conducted using PC3 and MCF7.1 human tumor cell lines. MCF7.1 is an in vivo selected line and originally derived from the parental human MCF7 breast cancer cell line. Cell lines are cultured in RPMI supplemented with 10% fetal bovine serum, 100 units/mL penicillin, and 100 μg/mL streptomycin, 10 mM HEPES, and 2 mM glutamine at 3°C under 5% CO2. MCF7.1 cells or PC3 cells are seeded in 384-well plates in media at 1000 cells/well or 3000 cells/well, respectively, and incubated overnight prior to the addition of GDC-0980 to a final DMSO concentration of 0.5% v/v. MCF7.1 cells and PC3 cells are incubated for 3 days and 4 days, respectively, prior to the addition of CellTiter-Glo reagen and reading of luminescence using an Analyst plate reader. For antiproliferative assays, a cytostatic agent such as aphidicolin and a cytotoxic agent such as staurosporine are included as controls. Dose−response curves are fit to a 4-parameter equation and relative IC50s are calculated using Assay Explorer software.
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  • 動物モデル: PC3 and MCF7.1 cells are injected s.c. into the right hind flank of athymic nu/nu (nude) mice.
  • 製剤: GDC-0980 is dissolved in 0.5% methylcellulose with 0.2% Tween-80 (MCT).
  • 投薬量: ≤7.5 mg/kg
  • 投与方法: Administered via p.o.

溶解度 (25°C)

体外 DMSO 20 mg/mL (40.11 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
体内 0.5% methylcellulose+0.2% Tween 80 30 mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。


分子量 498.6


CAS No. 1032754-93-0
in solvent
別名 GNE 390





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


マス 濃度 ボリューム 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01455493 Completed Endometrial Carcinoma Genentech, Inc. December 2011 Phase 2
NCT01487239 Completed Healthy Volunteer Genentech, Inc. December 2011 Phase 1
NCT01485861 Active, not recruiting Prostate Cancer Genentech, Inc. December 2011 Phase 1|Phase 2
NCT01473316 Completed Healthy Volunteer Genentech, Inc. November 2011 Phase 1
NCT01442090 Completed Renal Cell Carcinoma Genentech, Inc. October 2011 Phase 2
NCT01437566 Completed Breast Cancer Genentech, Inc. October 2011 Phase 2



Handling Instructions


  • * 必須


PI3K Inhibitors with Unique Features


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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID