OSU-03012 (AR-12)

製品コードS1106

OSU-03012 (AR-12)化学構造

分子量(MW):460.45

OSU-03012 (AR-12)は一種の有効な組替えのPDK-1阻害剤で、無細胞試験でIC50値が5 μMで、OSU-02067に作用する効果より2倍が高くなります。

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カスタマーフィードバック(3)

  • Serum-deprived HEK293-AT1A cells were pretreated with PD98059 (20 uM; 1 h) or OSU03012 (10 uM; 6 h) prior to 5 min stimulation with AngII (100 nm) or SII (50 uM). A, abundance of phospho-Akt T308 in whole cell detergent lysates. Representative phospho-Akt and total Akt immunoblots are shown above a bar graph depicting the mean ?S.E. of three biological replicates.

    J Biol Chem 2014 289(38), 26155-66. OSU-03012 (AR-12) purchased from Selleck.

    (C) Orbital fibroblasts, in this case from a patient with TAO, were transfected with PDK1siRNA while fibrocytes were treated with OSU-03012 (5 mM) for 6 h. Cultures were treated as indicated (bTSH, 5 mIU/mL) for 30 min. Cellular protein was subjected to Western blot analysis of PKCm and pPKCm in fibroblasts (left panel) and PKCbII and pPKCbII in fibrocytes (right panel). (D) Confluent cultures were pre-treated without or with OSU-03012 (5 mM) for 6 h, then treated with nothing (control) or bTSH (5 mIU/ml) for 30 min. Cellular proteins were subjected to Western blot analysis probing with AKT and pAKT antibodies. Inhibition of TSH-dependent pAKT by OSU-03012 in 3 separate experiments was 14.461.2% and 2.560.6% in fibroblasts and fibrocytes, respectively.

    PLoS One 2013 8, e75100. OSU-03012 (AR-12) purchased from Selleck.

  • Apoptosis is detectable in OSU-03012-treated Eca-109 cells. After treatment with or without 2 umol/l OSU-03012 for 24 h, Eca-109 cells were fixed for the TUNEL assay ( x 200).

    Anticancer Drugs 2013 24(7), 690-8. OSU-03012 (AR-12) purchased from Selleck.

製品安全説明書

PDK阻害剤の選択性比較

生物活性

製品説明 OSU-03012 (AR-12)は一種の有効な組替えのPDK-1阻害剤で、無細胞試験でIC50値が5 μMで、OSU-02067に作用する効果より2倍が高くなります。
特性 A derivative of celecoxib with 10-fold greater antitumor activity, but lacks celecoxib's COX-2 inhibitory activity.
ターゲット
PDK-1 [1]
(Cell-free assay)
5 μM
体外試験

OSU-03012 induces apoptotic death in PC-3 cells with IC50 of 5 µM and reduces the activity of immunoprecipitated p70S6K. OSU-03012 completely suppress cell growth in a diverse range of tumor cell lines at concentrations of 3–5 μm, as compared with the concentration of at least 50 μm required for celecoxib. [1] OSU-03012 promotes cell killing to a greater extent in glioma cells than in nontransformed astrocytes. OSU-03012 causes a dose-dependent induction of cell death that is not altered by p53 mutation, expression of ERBB1 VIII, or loss of phosphatase and tensin function due to a homolog deletion on chromosome 10. OSU-03012 and ionizing radiation cause an additive, caspase-independent elevation in cell killing. OSU-03012 lethality as a single agent or when combined with signaling modulators is not modified in cells lacking expression of BIM or of BAX/BAK. OSU-03012 promotes the release of cathepsin B from the lysosomal compartment and that of AIF from mitochondria. The lethality of OSU-03012 is attenuated in protein kinase R-like endoplasmic reticulum kinase-/- cells, which correlated with the reduced cleavage of BID and suppression of cathepsin B and AIF release into the cytosol. [2] OSU-03012 inhibits thyroid cancer cell (NPA, WRO, and ARO cells) proliferation, migration and induces apoptosis, which results in an increase of cells in the S phase without an increase of cells in G2. OSU-03012 is an ATP-competitive inhibitor of PAK activity and suppresses the phosphorylation of AKT in thyroid cancer cells. [3] OSU-03012 inhibits cell growth of hepatocellular carcinoma cell lines including Huh7, Hep3B and HepG2 cells with IC50 values below 1 μM. OSU-03012 does not suppress PDK1 or AKT activity or induce cellular apoptosis but induces autophagy in Huh7 cells. Moreover, accumulation of reactive oxygen species (ROS) is detected after OSU-03012 treatment. [4] A recent study shows that OSU-03012 could enhance the susceptibility of (Bcr)-Abl mutant cell lines to imatinib-induced apoptosis. [5]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse RAW264.7 cells NUi4XVFMTnWwY4Tpc44h[XO|YYm= NHroVHM5KGh? NH7NcolCdnSrbXnjdo9jcWGuIHHjeIl3cXS7IHHnZYlve3RiU3HscY9v\WyuYTDlcpRmemmlYTDz[ZJwfmG{IGT5dIhqdXW{aYXtJGFVS0NiMUSwNlghcW6oZXP0[YQhcW5ibX;1d4UhWkGZMk[0Mlch[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDpcpRz[WOnbHz1cIFzKGKjY4TldolidCCpcn;3eIgh[W[2ZYKgPEBpenNuIFnDOVA:OC5{IN88US=> M3PYdVE6QDB3NU[4
mouse RAW264.7 cells MmPzR5l1d3SxeHnjxsBie3OjeR?= MkToNlQhcA>? MXnDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVExKM7:TR?= NELPR4QyQThyNUW2PC=>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 OSU-03012 suppresses tumor growth by 57.59% and increases cleaved LC3 in Huh7 tumor xenografts at 200 mg/kg. [4] OSU-03012 remarkably decreases expression of EGFR protein in the tumors by 48% compared with vehicle controls and also prevents YB-1 from binding to the EGFR promoter in MDA-MB-435/LCC6 xenografts. [6] OSU-03012 is well tolerated and inhibits the growth of HMS-97 schwannoma xenografts by 55% after oral administration. [7]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
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PDK-1 Kinase Assay:

This in vitro assay is performed using a PDK-1 kinase assay kit. This cell-free assay is based on the ability of recombinant PDK-1, in the presence of DMSO vehicle or OSU-03012, to activate its downstream serum- and glucocorticoid-regulated kinase which, in turn, phosphorylates the Akt/serum- and glucocorticoid-regulated kinase-specific peptide substrate RPRAATF with [γ-32P]ATP. The 32P-phosphorylated peptide substrate is then separated from the residual [γ-32P]-ATP by using P81 phosphocellulose paper and quantitated in a scintillation counter after three washes with 0.75% phosphoric acid.
細胞試験: [1]
+ 展開
  • 細胞株: PC-3 cells
  • 濃度: 0-10 μM
  • 反応時間: ~72 hours
  • 実験の流れ: The effect of OSU-03012 on PC-3 cell viability is assessed by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide assay in six replicates. Cells are grown in 10% FBS- supplemented RPMI 1640 in 96-well, flat-bottomed plates for 24 hours. They are exposed to various concentrations of OSU-03012 (0-10 μM) dissolved in DMSO (final concentration ≤0.1%) in 1% serum-containing RPMI 1640 for different time intervals (~72 hours). Controls receive DMSO vehicle at a concentration equal to that in OSU-03012-treated cells. The medium is removed and replaced by 200 μL of 0.5 mg/mL 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide in 10% FBS-containing RPMI 1640. The cells are incubated in the CO2 incubator at 37 °C for 2 hours. Supernatants are removed from the wells, and the reduced 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide dye is solubilized in 200 μL DMSO per well. Absorbance at 570 nm is determined by using a plate reader.
    (参考用のみ)
動物試験:[4]
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  • 動物モデル: Huh7 tumor xenografts in male BALB/c nude mice
  • 製剤: Dissolved in 0.5% methylcellulose, 0.1% Tween 80
  • 投薬量: 100-200 mg/kg
  • 投与方法: Daily by gavage
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 11 mg/mL (23.88 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble
体内 順序で溶剤を入れること:
0.5% methylcellulose+0.2% Tween 80
30 mg/mL

* 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。

化学情報

分子量 460.45
化学式

C26H19F3N4O

CAS No. 742112-33-0
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

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

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

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00978523 Completed Solid Tumors|Lymphoma Arno Therapeutics August 2009 Phase 1

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

PDK信号経路図

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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