Onalespib (AT13387)


Onalespib (AT13387)化学構造


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.

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  • 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.


HSP (e.g. HSP90)阻害剤の選択性比較


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.
HSP90 [1]
(Cell-free assay)
18 nM

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]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HCT116 cells MU\DfZRwfG:6aXRCpIF{e2G7 NV\GbGN{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JGFt[W2jcjDicJVmKGG|c3H5MEBKSzVyPUCuNFQ5KM7:TR?= Mm[wNlA3PjJ3M{S=
human HCT116 cells NX\KPGNHWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXTG[IFPPDhiaB?= MlKwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkC4JO69VQ>? NVTjOY9JOjR5NkOyOlE>
human SKBR3 cells NUfvOHRGWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUW0PEBp MkjKRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1LSN{Bk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMUSg{txO MVWyOFc3OzJ4MR?=
human MCF7 cells MYHQdo9tcW[ncnH0bY9vKGG|c3H5 NHS0UXI1QCCq M{TLTmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMkig{txO MXuyOFc3OzJ4MR?=
human A231 cells NGT4UlNRem:uaX\ldoF1cW:wIHHzd4F6 NXjtNHlOPDhiaB?= MknKRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMkOxJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OS5yMTFOwG0> NXjINW1bOjR5NkOyOlE>
human HCT116 cells NH3UTY9HfW6ldHnvckBie3OjeR?= M4LNbFExKG6P MmnsNVghcA>? MVLJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gTJNxPzBibHX2[Ywh[XRiMUCgcm0h[W[2ZYKgNVghcHK|IHL5JIludXWwb3Lsc5R1cW6p M3\aWFIxPjZ{NUO0
human HCT116 cells NGPQepBHfW6ldHnvckBie3OjeR?= M1PzSlMxKG6P NUPHW|B{OThiaB?= MUjJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiQ1TLOEBt\X[nbDDheEA{OCCwTTDh[pRmeiBzODDodpMh[nliaX3teY5w[myxdITpcoc> M3\oOlIxPjZ{NUO0
human HCT116 cells MYjGeY5kfGmxbjDhd5NigQ>? MlPNN|Ahdk1? MXqxPEBp MV7JcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiUnHmMVEhdGW4ZXygZZQhOzBibl2gZYZ1\XJiMUigbJJ{KGK7IHntcZVvd2Kub4T0bY5o Mn[5NlA3PjJ3M{S=


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]


+ 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.
+ 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

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)

* 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。


分子量 409.52


CAS No. 912999-49-6
in solvent
別名 N/A





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


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


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

  • C1



  • 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):




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


質量 濃度 体積 分子量


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 Malignant Solid Neoplasm|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
NCT02627430 Withdrawn Adult Solid Neoplasm|Estrogen Receptor Negative|Fallopian Tube Serous Neoplasm|HER2/Neu Negative|Ovarian Serous Adenocarcinoma|Ovarian Serous Tumor|Primary Peritoneal Serous Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) March 2016 Phase 1
NCT02474173 Recruiting Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Stage III Breast Cancer AJCC v7|Stage IIIA Breast Cancer AJCC v7|Stage IIIB Breast Cancer AJCC v7|Stage IIIC Breast Cancer AJCC v7|Stage IV Breast Cancer AJCC v6 and v7|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) January 15 2016 Phase 1
NCT02535338 Active not recruiting EGFR Activating Mutation|EGFR Exon 20 Insertion Mutation|Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer AJCC v7 National Cancer Institute (NCI) January 21 2016 Phase 1|Phase 2



Handling Instructions


  • * 必須


  • 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