キナーゼ阻害剤ライブラリー

目录号 L1200

429種類のキナーゼ阻害剤の集めです。

サイズ 価格(税別)  
予めDMSOに溶解します
100uL/well (10mM solution) JPY 1171462.00
2x100uL/well (10mM solution) JPY 1794792.00
ご連絡ください

お気に入りの分子或いは調達サービスにより、分子ライブラリーをカスタマイズします。
お客様自分の特別なニーズに満たすために、お客様は弊社の製品を数量、状態(乾燥状態/固体或いはDMSO)等で選択できます。

キナーゼ阻害剤ライブラリー内容

お客様叙述(10)

  • The regressing tumour microenvironment stimulates the outgrowth, infiltration and metastasis of drug-resistant clones. b, Bioluminescent signal of drug-resistant A375RTGL cells in vemurafenib-sensitive, A375 tumours, treated with vehicle or vemurafenib for 5 days (vehicle, n = 36; vemurafenib, n = 15 tumours). D, day. c, EdU incorporation in A375R-TGL cells in A375/A375R-TGL tumours treated with vehicle or vemurafenib for 4 days, as determined by FACS (vehicle, n = 8; vemurafenib, n = 6 tumours). d, Bioluminescent signal of A375R-TGL tumours alone, treated with vehicle or vemurafenib for 5 days (vehicle, n 5 38; vemurafenib, n = 15 tumours). e, Bioluminescent signal of TGLexpressing drug-resistant cancer cells (A375R, M249R4, PC9 and H2030) in drug-sensitive tumours (Colo800, LOX, UACC62, M249, H3122 and HCC827) treated with vehicle or drugs (vemurafenib, crizotinib and erlotinib) for 5 days (n (from left to right on the graph) = 6, 7, 12, 12, 9, 9, 25, 26, 9, 12, 12, 12, 16 and 11 tumours). f, Spontaneous lung metastasis by A375R cells in mice bearing A375/A375R-TGL tumours treated with vehicle or vemurafenib (10 days), visualized by BLI (n = 4).

    Nature 2015 520(7547), 368-72. Vemurafenib (PLX4032, RG7204) purchased from Selleck

    FRA1 downregulation during RAFi treatment drives the reactive secretome. c, Relative mRNA levels of FRA1 during vemurafenib exposure [0.1-1 uM]. d, Representative immunofluorescence staining of A375/A375R tumours for GFP (A375R, green) and FRA1 (red) after vehicle or vemurafenib treatment (5 days). DAPI, 49,6-diamidino-2-phenylindole. Scale bars, 50 um.

    Nature 2015 520(7547), 368-72. Vemurafenib (PLX4032, RG7204) purchased from Selleck

  • Phosphorylation of PPARg in epididymal white adipose tissue in ob/ob mice after treatment with MEK inhibitors. Gene expression in ob/ob epididymal white adipose tissue after treatment with vehicle or either of two MEK inhibitors, PD0325901 or GSK1120212 (n = 7, 7 and 8, respectively). Areas under the curve and gene expression were analysed by analysis of variance.

    Nature 2015 517(7534), 391-5. PD0325901 purchased from Selleck

    SMYD3 knockout augments the effects of the MEK1/2 inhibitor Trametinib (GSK1120212) in vivo. Representative serial HE staining and IHC for pERK1/2, a marker of Ras activity, and MUC5, a marker of PanIN lesions. All scale bars, 50 um.

    Nature 2014 510(7504), 283-7. Trametinib (GSK1120212) purchased from Selleck

  • Targeting PI3K, a common downstream effector of RTKs, with a selective inhibitor (GDC0941) sensitizes SOX10 knockdown cells to vemurafenib. shRNAs targeting SOX10 were introduced into A375 cells by lentiviral transduction. pLKO.1 empty vector served as a control vector (Ctrl). Cells were seeded in 6-well plates at the same density in the presence or absence of drug(s) at the indicated concentration. Cells were cultured for 2 weeks in the absence of vemurafenib or 4 weeks in the presence of vemurafenib before fixing and staining.

    Nature 2014 508(7494), 118-22. Barasertib (AZD1152-HQPA) purchased from Selleck

    PDGF-AA induces Ezh2 expression and proliferation in juvenile islets but not in adult islets. Western immunoblots of indicated islet proteins from 3 week or 9 month-old WT islets 2 days after exposure to PDGF-AA alone, or PDGF-AA plus RTK inhibitors Sunitinib.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck

  • Assessment of effects on human juvenile or adult islets after exposure to PDGF-AA (50 ng/ml) for 2 days, with or without Sunitinib (2 uM) or U0126 (10 uM)co-treatment. Average percentage of BrdU+ insulin+ cells was morphometry from sectioned islets immunostained for insulin (green), glucagon (white) and BrdU (red). n = 3-6 independent experiments.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck

    Survival curves for isogenic cell line pairs and melanoma cultures treated with the indicated AZD6244 concentration for 72 h (relative to DMSO treated controls; mean6s.e.m., n55). PLX4032 resistant cells were grown with PLX4032. Dashed line, 50% cell killing.

    Nature 2010 468, 973-977. Selumetinib (AZD6244) purchased from Selleck

  • A,ERK phosphorylation in A375 expressing indicated ORFs following treatment with DMSO or 1 μM of PLX4720, RAF265, CI-1040 or AZD6244. B,ERK phosphorylation in A375 expressing indicated ORFs following treatment with DMSO, PLX4720 (1 μM) or PLX4720 in combination with CI-1040 or AZD6244 (all 1 μM).

    Nature 2010 468, 968-972. Selumetinib (AZD6244) purchased from Selleck

    Protein blots showing MYC expression in naive and persister cells after 3 d of treatment with 2 uM AKT inhibitor MK-2206 (AKTi) or 10 nM mTOR inhibitor rapamycin (Rapa).

    Nat Genet 2014 46(4), 364-70. Rapamycin (Sirolimus) purchased from Selleck

製品特性&メリット

• 429種類のキナーゼ阻害剤の集めです。これをHTSとHCS (high content screening) に使用できます。
• 前期臨床研究と臨床試験を通じて、生物活性と安全性が検証されました。
• 若干のキナーゼ阻害剤はFDAに認証されました。
• キナーゼ(例えばRTK、PI3K、オーロラ・キナーゼ、cdkとMEK)に作用します
• 大部分はATP競争性抑制剤です。
• 構造多様で、効果が目立って、細胞浸透可。
• 十分に詳しい構造説明、,IC50値とお客様からフィードバックした資料があります。
• NMRとHPLC技術で製品の高純度を保証します。

製品詳細情報

調合: 429種類のキナーゼ阻害剤はDMSO溶液に溶解します
96穴板: 96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode
安定性: in DMSO
in DMSO
出荷方式: ブルーアイス物流
包装: 不活性ガス(Inert gas)

キナーゼ阻害剤ライブラリー製品説明

Kinase Inhibitor Library Composition

HTS パートナ

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