Onalespib (AT13387)

製品コードS1163

Onalespib (AT13387)化学構造

分子量(MW):409.52

Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2.

サイズ 価格(税別)  
JPY 73040.00
JPY 44820.00
JPY 61420.00

カスタマーフィードバック(3)

  • Relative effect of pharmacological HSP90 inhibition by (B) onalespib (AT13387, 10-40 nM) on the viability of FANCA wild-type and FANCA null cells under normal conditions or with increasing concentrations of MMC. Left panels indicate the effects of the indicated inhibitor on cell growth; middle panels the effects onMMCtolerance in FANCA-wild-type cells; right panels the effects onMMCtolerance in FANCA null cells Data presented as the mean ± SEM from 2 independent experiments.

    Cell, 2017, 168(5):856-866. Onalespib (AT13387) purchased from Selleck.

    The cultured cells were pretreated with the indicated doses of onalespib for 60 min, and then stimulated by 10 μM of PGF2α or vehicle for 10 min. The cell extracts were then subjected to SDS-PAGE with subsequent Western blot analysis with antibodies against phospho-specific p38 MAP kinase or p38 MAP kinase. The histogram shows the quantitative representations of the levels of phosphorylated p38 MAP kinase after normalization with respect to p38 MAP kinase obtained from laser densitometric analysis. The levels were expressed as the fold increase to the basal levels presented as lane 1. Each value represents the mean ± S.E.M. of triplicate determinations from three independent cell preparations. *p<0.05 compared to the value of control. **p<0.05 compared to the value of PGF2α alone.

    PLoS One, 2017, 12(5):e0177878. Onalespib (AT13387) purchased from Selleck.

  • IC50 determinations of compound S1 and S13 on heat shock poteins ATPase activity using ADP fluorescence assay. (A) inhibition of HSP70 (B) inhibition of HSP90 The test compounds were diluted from mother plates (10 mM in 100% (v/v) DMSO) into series of concentration (in 2.0% (v/v) DMSO). AT13387 and 17-DMAG were used as positive controls in each assay. Data were performed in triplicate and analyzed by GraphPad.Prism.

    PLoS One 2013 8, e59315. Onalespib (AT13387) purchased from Selleck.

製品安全説明書

HSP (e.g. HSP90)阻害剤の選択性比較

生物活性

製品説明 Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2.
ターゲット
HSP90 [1]
(Cell-free assay)
18 nM
体外試験

The Kd for AT13387 binding is 0.7 nM. This compares to a Kd of 6.7 nM for the binding of the ansamycin 17-AAG to the same site. The mean stoichio metry of binding for AT13387 is 1.03. The inhibition of a number of isolated kinases by AT13387 is also investigated including CDK 1, CDK 2, CDK4, FGFR3, PKB-b, JAK2, VEGFR2, PDGFRβ and Aurora B. None of the tested kinases are significantly inhibited at concentrations below 30 μM. AT13387 is a potent inhibitor of the proliferat ion and survival of many different cell lines (such as MES-SA cell line) from a variety of different tumor types. Across a panel of 30 tumor cell lines, AT13387 potently inhibits cell proliferation with GI50 values in the range 13-260 nM. AT13387 inhibits proliferation of the non-tumorigenic human prostate epithelial cell line PNT2 with a GI50 value of 480 nM. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HCT116 cells NFXuPHFEgXSxdH;4bYPDqGG|c3H5 NUXoZYVxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JGFt[W2jcjDicJVmKGG|c3H5MEBKSzVyPUCuNFQ5KM7:TR?= NFvtSogzODZ4MkWzOC=>
human HCT116 cells MVXQdo9tcW[ncnH0bY9vKGG|c3H5 NEjFRW01QCCq NY\rTpBtSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA5KM7:TR?= NGOwOI8zPDd4M{K2NS=>
human SKBR3 cells M13CRnBzd2yrZnXyZZRqd25iYYPzZZk> MUC0PEBp M{O1TmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vCVlMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkG0JO69VQ>? NGjGcoYzPDd4M{K2NS=>
human MCF7 cells NGTDfmxRem:uaX\ldoF1cW:wIHHzd4F6 Mn7kOFghcA>? Mkj2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5{ODFOwG0> MnOwNlQ4PjN{NkG=
human A231 cells MlTqVJJwdGmoZYLheIlwdiCjc4PhfS=> Mn7COFghcA>? MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF{M{GgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjBzIN88US=> M1zDTVI1PzZ|Mk[x
human HCT116 cells NFvoR|NHfW6ldHnvckBie3OjeR?= NXjwTJQzOTBibl2= NVrKNnlWOThiaB?= MoG5TY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJGh{eDdyIHzleoVtKGG2IEGwJI5OKGGodHXyJFE5KGi{czDifUBqdW23bn;icI91fGmwZx?= MVOyNFY3OjV|NB?=
human HCT116 cells MYHGeY5kfGmxbjDhd5NigQ>? NUPJVG41OzBibl2= M3HaVVE5KGh? NFiz[oxKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gR2RMPCCuZY\lcEBifCB|MDDuUUBi\nSncjCxPEBpenNiYomgbY1ufW6xYnzveJRqdmd? NFWzSlczODZ4MkWzOC=>
human HCT116 cells NHfpc4lHfW6ldHnvckBie3OjeR?= MV6zNEBvVQ>? NXTRSWpGOThiaB?= NXTnTm8yUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJHJi\i1zIHzleoVtKGG2IEOwJI5OKGGodHXyJFE5KGi{czDifUBqdW23bn;icI91fGmwZx?= NXLING04OjB4NkK1N|Q>

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 When given on an intermittent basis, AT13387 could be tolerated at doses of up to 70 mg/kg twice weekly or 90 mg/kg once weekly. Body weight loss in mice does not exceed 20% before recovering in all cases except one, and loss is highest following the second dose. Tumor growth inhibition is similar in NCI-H1975 for both dosing regimens. The maintenance of antitumor effects with such a prolonged off-treatment period is consistent with the extended pharmacodynamic action of AT13387 observed for mutant EGFR and other biomarkers in vitro and in vivo and the extended retention of AT13387 in tumors. [2]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[2]
+ 展開

HSP90 competition isothermal calorimetry:

Kd values for AT13387 binding to HSP90 are determined with a competition Isothermal Calorimetry (ITC) format. ITC experiments are performed on a Micro Cal VP-ITC at 25 °C in a buffer comprising 25 mM Tris, 100 mM NaCl, 1 mM MgCl2 and 1 mM Tris(2-carboxy- ethyl)phosphine at pH 7.4 in order to maintain the higher affinit
細胞試験: [2]
+ 展開
  • 細胞株: A375, 22RV1 and T474 cells
  • 濃度: 1 μM
  • 反応時間: 4 hours
  • 実験の流れ: The human cell lines including A375, 22RV1, T474, DU1 45, LNCa P, MCF-7, DA-MB-468 are seeded into 96-well plates before the addition of AT13387 in 0.1% (v/v) DMSO. GI50 are determined using a 10-point dose response curve for three cell doubling times. After AT13387 incubation 10% (v/v), Alamar blueis added, and cells are incubated for a further 4 hours. Fluorescence is read.
    (参考用のみ)
動物試験:[2]
+ 展開
  • 動物モデル: Athymic BALB /c mice
  • 製剤: 17.5% cyclodextrin
  • 投薬量: 80 mg/kg
  • 投与方法: Intraperitoneal adminis tration
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 25 mg/mL (61.04 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% PEG 300+ddH2O (prepare before use)
混合させたのち直ちに使用することを推奨します。
10mg/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 409.52
化学式

C24H31N3O3

CAS No. 912999-49-6
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
NCT02898207 Recruiting Estrogen Receptor Negative|HER2/Neu Negative|High Grade Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Metastatic Breast Carcinoma|Metastatic Malignant Solid Neoplasm|Platinum-Resistant Fallopian Tube Carcinoma|Platinum-Resistant Ovarian Carcinoma|Platinum-Resistant Primary Peritoneal Carcinoma|Primary Peritoneal High Grade Serous Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma|Unresectable Malignant Solid Neoplasm National Cancer Institute (NCI) May 19 2017 Phase 1
NCT02898207 Recruiting Estrogen Receptor Negative|HER2/Neu Negative|High Grade Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Metastatic Breast Carcinoma|Metastatic Malignant Solid Neoplasm|Platinum-Resistant Fallopian Tube Carcinoma|Platinum-Resistant Ovarian Carcinoma|Platinum-Resistant Primary Peritoneal Carcinoma|Primary Peritoneal High Grade Serous Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma|Unresectable Malignant Solid Neoplasm National Cancer Institute (NCI) May 19 2017 Phase 1
NCT02572453 Recruiting ALK Positive|BCL6 Positive|Recurrent Anaplastic Large Cell Lymphoma|Recurrent Diffuse Large B-Cell Lymphoma|Recurrent Mantle Cell Lymphoma|Refractory Anaplastic Large Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma|Refractory Mantle Cell Lymphoma National Cancer Institute (NCI) April 4 2016 Phase 2
NCT02503709 Recruiting Advanced Malignant Solid Neoplasm|Metastatic Malignant Solid Neoplasm|Unresectable Solid Neoplasm National Cancer Institute (NCI) April 8 2016 Phase 1
NCT02572453 Recruiting ALK Positive|BCL6 Positive|Recurrent Anaplastic Large Cell Lymphoma|Recurrent Diffuse Large B-Cell Lymphoma|Recurrent Mantle Cell Lymphoma|Refractory Anaplastic Large Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma|Refractory Mantle Cell Lymphoma National Cancer Institute (NCI) April 4 2016 Phase 2
NCT02503709 Recruiting Advanced Malignant Solid Neoplasm|Metastatic Malignant Solid Neoplasm|Unresectable Solid Neoplasm National Cancer Institute (NCI) April 8 2016 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

よくある質問(FAQ)

  • 質問1:

    How to prepare the compound for in vivo studies?

  • 回答:

    S1163 AT13387 can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as a clear solution. But after stayed for about 1 hour, the precipitation will goes out. So it is recommended to be prepared before use.

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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