Rabusertib (LY2603618)

製品コードS2626 別名:IC-83

Rabusertib (LY2603618)化学構造

分子量(MW):436.3

Rabusertib (LY2603618) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated.

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

カスタマーフィードバック(6)

  • MK-1775 and LY2603618 synergize to induce apoptosis in AML cell lines and primary patient samples. U937 and CTS cells were treated for 8 h. Whole cell lysates were subjected to Western blotting and probed with anti-γH2AX, -pCHK1, -p-cdc25c, -p-CDK1, -p-CDK2, -CDK1, or -β-actin antibody. Densitometry measurements, as described in the Materials and methods section, are shown below the corresponding Western blot.

    J Hematol Oncol 2014 7, 53. Rabusertib (LY2603618) purchased from Selleck.

    BxPC-3 cells were treated with vehicle control, MK-1775 (MK), LY2603618 (LY) or MK-1775 plus LY2603618 for 48 h. Protein extracts were subjected to Western blotting and probed with anti-PARP, -p-CHK1, -CHK1, -p-CDC25C, -p-CDK1, -CDK1, -p-CDK2, -CDK2, -γH2AX, or -β-actin antibody.

    Cancer Lett 2014 10.1016/j.canlet.2014.10.015. Rabusertib (LY2603618) purchased from Selleck.

  • Biomarker changes induced in response to gemcitabine plus Chk1 inhibitor treatment in HT29 colon carcinoma cells. HT29 colon cancer cells were exposed to 50 nM gemcitabine (+) for 16 hours followed by increasing concentrations of Chk1 inhibitor for a further 24 hours. Protein expression was characterized by immunoblotting.

    BMC Cancer 2014 14, 483. Rabusertib (LY2603618) purchased from Selleck.

    Oncol Rep, 2018, 39(3):1322-1330. Rabusertib (LY2603618) purchased from Selleck.

  • C6 cell was trypsinized and plated at 30% confluence in DMEM. 16 hours later, LY2603618 was added at final concentrations of 0, 1, 5, 10 and 20uM. Another 24 hours later, cells were harvested in RIPA with protease and phosphatase inhibitor cocktail. Total protein concentration was measured by BCA method. Lysates equivalent to 20ug total protein were subject to Western Blot, using pS345-CHK1, g-H2AX and beta-actin (internal control) antibodies.

    Customer W, F. Z. Rabusertib (LY2603618) purchased from Selleck.

    Hela cell was trypsinized and plated at 30% confluence in DMEM. 16 hours later, LY2603618 was added at final concentrations of 0, 5, 10 and 25uM. Another 24 hours later, cells were harvested in RIPA with protease and phosphatase inhibitor cocktail. Total protein concentration was measured by BCA method. Lysates equivalent to 20ug total protein were subject to Western Blot, using total- CHK1, pS345-CHK1 and beta-actin (internal control) antibodies.

    Rabusertib (LY2603618) purchased from Selleck.

製品安全説明書

Chk阻害剤の選択性比較

生物活性

製品説明 Rabusertib (LY2603618) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated.
ターゲット
Chk1 [1]
(Cell-free assay)
7 nM
体外試験

Chk1 is an ATP-dependent serine-threonine kinase and a key component in the DNA replication-monitoring checkpoint system activated by double-stranded breaks (DSBs). Chk1 contributes to all currently defined cell cycle checkpoints, including G1/S, intra-S-phase, G2/M, and the mitotic spindle checkpoint. By inhibiting the activity of chk1, LY2603618 prevents the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. However, preclinical data involving LY2603618 has not been published until now. [1] Inhibition of Chk1 is predicted to enhance the effects of antimetabolites, such as gemcitabine. [2] LY2603618 treatment impairs DNA synthesis, increases DNA damage (via mitotic defects), induces apoptosis, and has synergistic activity with pemetrexed, especially in p53 mutant tumor cells. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT474 NYDvTpFFU2mwYYPlJIF{e2G7 M3zFNFEh|ryP M1f1UGROW09? NXfOdFNNcW6qaXLpeJMhWC2FSFuxJIxmfmWucx?= Mm\GNlM6OTd|N{i=
MCF7 MXHLbY5ie2ViYYPzZZk> NW\zXHlDOSEQvF2= MoLkSG1UVw>? MnzPbY5pcWKrdIOgVE1EUEtzIHzleoVtew>? NF\C[WgzOzlzN{O3PC=>
Hela NHTSbZNMcW6jc3WgZZN{[Xl? NHnCSnM{OzByIH7N NETCe3hFVVOR MUnpcohq[mm2czDDbIsyKGGldHn2bZR6 MWiyOFEyPDF{NB?=
Calu6 NUjFVIJxU2mwYYPlJIF{e2G7 MXezN|AxKG6P NWi2VGV5TE2VTx?= MVPpcohq[mm2czDDbIsyKGGldHn2bZR6 NXvoZXZWOjRzMUSxNlQ>
A549 Mm\RSpVv[3Srb36gZZN{[Xl? M2iyOZ4yOCEQvF2= Ml;KSG1UVw>? NYLjXmltcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MXmyOFkzQDJyNR?=
H1299 MmrkSpVv[3Srb36gZZN{[Xl? MV7+NVAh|ryP M3T2cmROW09? MlrubY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MkLkNlQ6Ojh{MEW=
A549 NFjtUo9HfW6ldHnvckBie3OjeR?= NXW2NFBqhjJyIN88US=> NFTDRVRFVVOR MlXxZYN1cX[jdHXzJGRPSSCmYX3h[4Uhe2Wwc3;yJItqdmG|ZYO= MX2yOFkzQDJyNR?=
H1299 NHX6eIJHfW6ldHnvckBie3OjeR?= M{jOPJ4zOCEQvF2= MlvQSG1UVw>? MnriZYN1cX[jdHXzJGRPSSCmYX3h[4Uhe2Wwc3;yJItqdmG|ZYO= NVv6OWh6OjR7MkiyNFU>
A549 NUThZmEzSXCxcITvd4l{KGG|c3H5 NIfjNG1,OjBizszN M3LBNGROW09? NGfiTHhqdmS3Y3XzJIFxd3C2b4Ppdy=> MkS4NlQ6Ojh{MEW=
H1299 NGPuRWJCeG:ydH;zbZMh[XO|YYm= NYnUSnRKhjJyIN88US=> NFzl[YZFVVOR NIfNflhqdmS3Y3XzJIFxd3C2b4Ppdy=> M1zkelI1QTJ6MkC1
A549 NIjKflhEgXSxeHnjbZR6KGG|c3H5 M{P1[J4zOCEQvF2= M164U2ROW09? M2HEOolv\HWlZYOgZZV1d3CqYXf5 MWOyOFkzQDJyNR?=
H1299 NHTv[2hEgXSxeHnjbZR6KGG|c3H5 Mli2glIxKM7:TR?= M1G0cGROW09? MWjpcoR2[2W|IHH1eI9xcGGpeR?= MojUNlQ6Ojh{MEW=
A549 NIL5c4NHfW6ldHnvckBie3OjeR?= MVH+NlAh|ryP MXHEUXNQ MXTpcoNz\WG|ZYOgTm5MKGGwZDDwN|ghVUGSSzDwbI9{eGixconsZZRqd25? NIW4WY4zPDl{OEKwOS=>
H1299 MnHSSpVv[3Srb36gZZN{[Xl? MYP+NlAh|ryP M2WxSmROW09? NX\HNmZwcW6lcnXhd4V{KEqQSzDhcoQheDN6IF3BVGsheGixc4Doc5J6dGG2aX;u MYKyOFkzQDJyNR?=

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 In xenograft models, LY2603618 delays tumor growth when given in combination with pemetrexed. [3]

お薦めの試験操作(参考用のみ)

細胞試験:

[4]

+ 展開
  • 細胞株: A549 and H1299 cell
  • 濃度: 5 or 10 μM
  • 反応時間: 24 h
  • 実験の流れ:

    Cells were treated with LY2603618 and DMSO as a control. After trypsinization, cells were fixed in 70 % ethanol at 4 C overnight. The cells were washed twice with PBS and incubated for 30 min in the dark in PBS containing propidium iodide (PI) and RNase A. Stained cells were analyzed by a FACScan flow cytometry and CellQuest analysis software.


    (参考用のみ)

溶解度 (25°C)

体外 DMSO 13 mg/mL (29.79 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):
2% DMSO+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。
30mg/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 436.3
化学式

C18H22BrN5O3

CAS No. 911222-45-2
保管
in solvent
別名 IC-83

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
NCT01358968 Completed Cancer Eli Lilly and Company June 2011 Phase 1
NCT01341457 Completed Solid Tumors Eli Lilly and Company May 2011 Phase 1
NCT01296568 Completed Advanced Cancer Eli Lilly and Company February 2011 Phase 1
NCT01139775 Completed Non Small Cell Lung Cancer Eli Lilly and Company February 2011 Phase 1|Phase 2
NCT00988858 Completed Non Small Cell Lung Cancer Eli Lilly and Company November 2009 Phase 2
NCT00839332 Completed Pancreatic Neoplasms Eli Lilly and Company February 2009 Phase 1|Phase 2

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

Chkシグナル伝達経路

Chk Inhibitors with Unique Features

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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