AEE788 (NVP-AEE788)

製品コードS1486

AEE788 (NVP-AEE788)化学構造

分子量(MW):440.58

AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.

サイズ 価格(税別)  
JPY 49800.00
JPY 28220.00
JPY 53120.00
JPY 94620.00
JPY 161020.00

カスタマーフィードバック(2)

  • EGFR-SGLT1 interaction is irresponsive to modulators of EGFR’s tyrosine kinase. A: Immunoprecipitation coupled Western blot analysis ofinteractionsbetween EGFR-HA and SGLT1-FlaginHEK293 cells treatedwith EGF or AEE788. EGFR, total EGFR; pEGFR, phosphorylated EGFR; IP, immunoprecipitation; IB, immunoblot. Input, expression levels of indicated exogenous proteinsin HEK293 whole celllysates used for the IP.

    The Prostate, 2013, 73:1453-1461.. AEE788 (NVP-AEE788) purchased from Selleck.

    Representative images of mitochondria of PC3 cells treated with DMSO, EGF (20 ng/ml) AEE788 (a small molecular EGFR inhibitor at 6 μM) or AEE788+EGF for 24 h. Mitochondria were stained with Mitotracker Red and images were taken with a confocal microscope.

    Cell Cycle, 2014, 13(15):2415-30. AEE788 (NVP-AEE788) purchased from Selleck.

製品安全説明書

EGFR阻害剤の選択性比較

生物活性

製品説明 AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.
ターゲット
EGFR [1]
(Cell-free assay)
HER2/ErbB2 [1]
(Cell-free assay)
c-Abl [1]
(Cell-free assay)
FLT1 [1]
(Cell-free assay)
c-Fms [1]
(Cell-free assay)
2 nM 6 nM 52 nM 59 nM 60 nM
体外試験

AEE788 also inhibits KDR, c-abl, c-Src, and Flt-1 with IC50 of 50-80 nM. AEE788 is not sensitive to ErbB-4, PDGFR-β, Flt-3, Flt-4, RET, and c-Kit and has no inhibitory to Ins-R, IGF-1R, PKC-α, and PKA. AEE788 potently inhibits EGFR phosphorylation in A431 cells with IC50 of 11 nM. AEE788 also inhibits the phosphorylation of KDR in CHO cells and erbB2 in BT-474 cells, without any effects on PDGF-induced phosphorylation in A31 cells. AEE788 inhibits the proliferation of NCI-H596, MK, BT-474 and SK-BR-3 cells with IC50 of 78, 56, 49 and 381 nM, respectively. Otherwise, AEE788 has the additional property of inhibiting cellular proliferation driven by EGFR mutant including 32D/EGFR and 32D/EGFRvIII. AEE788 furtheralso inhibits both EGF- and VEGF-driven HUVEC proliferation with IC50 of 43 and 155 nM, respectively. [1] AEE788 inhibits the phosphorylation of EGFR, VEGFR2, Akt, and MAPK in human cutaneous SCC cell lines (Colo16, HaCaT, SRB1, and SRB12 cells), which leads to growth inhibition and induction of apoptosis. [2] AEE788 inhibits the phosphorylation of EGFR and Akt in HT29 cells at 0.2 to 1.0 μM. [3] AEE788 inhibits cell proliferation and prevents EGF- and neuregulin-induced HER1, HER2, and HER3 activation in medulloblastoma cell lines. AEE788 shows growth-suppressive activities in chemosensitive and chemoresistant medulloblastoma cells. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Huh7 NYTwb3RES3m2b4TvfIlkcXS7IHHzd4F6 M1\tfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJIhmeGG2b3PlcIx2dGG{IHPhdoNqdm:vYTDj[YxtKGyrbnWgLGh2cDdrLDDDR|UxRTJ5LkizJO6ddQ>? M{HaUVE5PTd7N{iz
Jeko B cells M2D0SmZ2dmO2aX;uJIF{e2G7 MljONkBp NEnJR5RKdmirYnn0bY9vKG:oIGDJN2tl\Wy2YTDpckBpfW2jbjDK[YtwKEJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBCc3RicHjvd5Bpd3K7bHH0bY9vKGGodHXyJFIhcHK|LDDJR|UxRTBwMEG3JO69VQ>? NIjacHkzPTVzNE[1PC=>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 AEE788 produces a dose-dependent inhibition of tumor growth in NCI-H596 or DU145 xenograft models, with only minor body weight changes. AEE788 induces tumor regression by 57% at 50 mg/kg in the NeuT/erbB2 GeMag model. AEE788 potently inhibits EGF-induced EGFR phosphorylation in A431 tumors and erbB2 phosphorylation in GeMag tumors. AEE788 dose-dependently inhibited angiogenesis induced by VEGF and does not inhibit bFGF-induced angiogenesis. [1] AEE788 suppresses the growth of tumor volume by 54% in Colo16 xenografts at 50 mg/kg, which dues to the inhibition of phosphorylation of EGFR, VEGFR, Akt, and MAPK. [2] AEE788 (50 mg/kg) also inhibits growth of tumors in the cecum and peritoneum (>50%) and reduces the incidence of lymph node metastasis to 70% in HT29 cells implanted in the cecum of nude mice, without loss of body weight and gross evidence of neovascularization. AEE788 significantly lowers the expression levels of pEGFR and pVEGFR in HT29 cecal tumors and does not alter those of EGF, VEGF, EGFR, or VEGFR. Combined with CPT-11, AEE788 has significantly smaller tumors and complete inhibition of lymph node metastasis. [3] AEE788 inhibits the growth of Daoy, DaoyPt, and DaoyHER2 xenografts by 51%, 45%, and 72%, respectively. [4] AEE788 could promote LBH589-mediated generation of reactive oxygen species in K562 tumor cells, which in turn increase apoptosis. [5]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
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Protein Kinase Assays:

The in vitro kinase assays are performed in 96-well plates (30 μL) at ambient temperature for 15–45 min using the recombinant glutathione S-transferase-fused kinase domains (4-100 ng, depending on specific activity). [γ33P]ATP is used as phosphate donor and polyGluTyr-(4:1) peptide as acceptor. With the exception of protein kinase C-α, cyclin-dependent kinase 1/cycB and protein kinase A are protamine sulfate (200 μg/mL), histone H1 (100 μg/mL), and the heptapeptide Leu-Arg-Arg-Ala-Ser-Leu-Gly (known as Kemptide Bachem) respectively and are used as peptide substrates. Assays are optimized for each kinase using the following ATP concentrations: 1.0 μM (c-Kit, c-Met, c-Fms, c-Raf-1, and RET), 2.0 μM (EGFR, erbB2, ErbB3, and ErbB4), 5.0 μM (c-abl), 8.0 μM (Flt-1, Flt-3, Flt-4, Flk, KDR, FGFR-1, and Tek), 10.0 μM (PDGFR-β, protein kinase C-α, and cyclin-dependent kinase 1), and 20.0 μM (c-Src and protein kinase A). The reaction is terminated by the addition of 20 μL 125 mM EDTA. Thirty μL (c-abl, c-Src, insulin-like growth factor-1R, RET-Men2A, and RET-Men2B) or 40 μL (all other kinases) of the reaction mixture is transferred onto Immobilon-polyvinylidene difluoride membrane, presoaked with 0.5% H3PO4 and mounted on a vacuum manifold. Vacuum is then applied and each well rinsed with 200 μL 0.5% H3PO4. Membranes are removed and washed four times with 1.0% H3PO4 and once with ethanol. Dried membranes are counted after mounting in a Packard TopCount 96-well frame and with the addition of 10 μL/well of Microscint. IC50 values (±SE) are calculated by linear regression analysis of the percentage inhibition and are averages of at least three determinations.
細胞試験: [1]
+ 展開
  • 細胞株: T24, BT-474, SK-BR-3, and NCI-H596 cells
  • 濃度: ~10 μM
  • 反応時間: 4 or 6 days
  • 実験の流れ: Methylene Blue Cell Proliferation Assay.Cells are seeded at 1.5 × 103 cells/well into 96-well microtiter plates and incubated overnight at 37 °C, 5% v/v CO2 and 80% relative humidity. AEE788 dilutions are added on day 1, with the highest concentration being 10 μM. After incubation of the cell plates for an additional 4 (T24) or 6 (BT-474, SK-BR-3, and NCI-H596) days, cells are fixed with 3.3% v/v glutaraldehyde, washed with water, and stained with 0.05% w/v methylene blue. After washing, the dye is eluted with 3% HCl and the absorbance measured at 665 nm with a SpectraMax 340 spectrophotometer. IC50 values are determined by mathematical curve-fitting and are defined as the drug concentration leading to 50% inhibition of net cell mass increase compared with untreated control cultures.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: NCI-H596, DU145, A431, B16 and oncogenic NeuT-transfected HC11 cells in female BALB/c nu/nu (nude) mice
  • 製剤: N-methylpyrrolidone and PEG300 1:9 (v/v)
  • 投薬量: 50 mg/kg
  • 投与方法: Dosed orally
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 88 mg/mL (199.73 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% PEG400+0.5% Tween80+5% propylene glycol
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 440.58
化学式

C27H32N6

CAS No. 497839-62-0
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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

希釈の計算式

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

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

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

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00116376 Completed Glioblastoma Multiforme Novartis Pharmaceuticals|Novartis January 2004 Phase 1|Phase 2
NCT00116376 Completed Glioblastoma Multiforme Novartis Pharmaceuticals|Novartis January 2004 Phase 1|Phase 2
NCT00107237 Completed Brain and Central Nervous System Tumors Novartis Pharmaceuticals|Novartis October 2003 Phase 1|Phase 2
NCT00107237 Completed Brain and Central Nervous System Tumors Novartis Pharmaceuticals|Novartis October 2003 Phase 1|Phase 2
NCT00118456 Completed Cancer Novartis Pharmaceuticals|Novartis July 2003 Phase 1
NCT00118456 Completed Cancer Novartis Pharmaceuticals|Novartis July 2003 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

EGFRシグナル伝達経路

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID