Onalespib (AT13387)

For research use only.

Catalog No.S1163

14 publications

Onalespib (AT13387) Chemical Structure

CAS No. 912999-49-6

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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Selleck's Onalespib (AT13387) has been cited by 14 publications

3 Customer Reviews

  • 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.

  • 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.

  • 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.

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Biological Activity

Description 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
In vitro

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HCT116 cells MnTQR5l1d3SxeHnjxsBie3OjeR?= M4LnWWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCkeTDBcIFu[XJiYnz1[UBie3OjeTygTWM2OD1yLkC0PEDPxE1? M3;w[lIxPjZ{NUO0
human HCT116 cells MnTMVJJwdGmoZYLheIlwdiCjc4PhfS=> NG\Zb2U1QCCq MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMEig{txO NEfye48zPDd4M{K2NS=>
human SKBR3 cells NUHEV45kWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1r3d|Q5KGh? M4TzeGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vCVlMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkG0JO69VQ>? MXuyOFc3OzJ4MR?=
human MCF7 cells NIPIbZhRem:uaX\ldoF1cW:wIHHzd4F6 M2TqSVQ5KGh? NFLidpZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkK4JO69VQ>? M1:wUlI1PzZ|Mk[x
human A231 cells MkjhVJJwdGmoZYLheIlwdiCjc4PhfS=> MlrHOFghcA>? NV:zZZUzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlMyKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT6wNUDPxE1? M4Kwc|I1PzZ|Mk[x
human HCT116 cells NIrHb4NHfW6ldHnvckBie3OjeR?= M3HlXVExKG6P MXOxPEBp NW\zO4c4UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNidYDy[Yd2dGG2aX;uJI9nKEi|cEewJIxmfmWuIHH0JFExKG6PIHHmeIVzKDF6IHjyd{BjgSCrbX31co9jdG:2dHnu[y=> NF7rSJIzODZ4MkWzOC=>
human HCT116 cells NYPCZ|N5TnWwY4Tpc44h[XO|YYm= MoH3N|Ahdk1? MX:xPEBp NGXOV25KdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gR2RMPCCuZY\lcEBifCB|MDDuUUBi\nSncjCxPEBpenNiYomgbY1ufW6xYnzveJRqdmd? MlvqNlA3PjJ3M{S=
human HCT116 cells MlPPSpVv[3Srb36gZZN{[Xl? NV;iT4R2OzBibl2= NGP3NYwyQCCq M1WyRWlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDSZYYuOSCuZY\lcEBifCB|MDDuUUBi\nSncjCxPEBpenNiYomgbY1ufW6xYnzveJRqdmd? M1PvVVIxPjZ{NUO0

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
HSP90 / HSP70 ; 

PubMed: 28679777     

HSP90 and HSP70 protein expression (upper panel) were evaluated by immunoblotting after treatment with onalespib 0.1, 0.2 and 0.4 μM for 48h on LN229, U251HF and A172 cell lines; GAPDH was used as loading control (lower panel). Immunoblots are representative of three independent experiments and DMSO was used as vehicle control.

EGFR / p-EGFR / AKT / p-AKT / ERK / p-ERK / S6 / p-S6 ; 

PubMed: 28679777     

LN229, U251HF and A172 cells were exposed to 0.1, 0.2 and 0.4 μM onalespib for 48 h before being evaluated for the expression of EGFR, pEGFR, AKT, pAKT, ERK1/2, p-ERK1/2, S6, p-S6 by immunoblotting. GAPDH was assayed as a loading control.

AXL / c-Myc / p-Mnk1 / Mnk1 / p-eIF4E / eIF4E ; 

PubMed: 31431614     

Immunoblots of A549 and A549R cells treated with onalespib for the indicated time. 

28679777 31431614
Growth inhibition assay
Cell viability; 

PubMed: 28679777     

MES (GSC2 and GSC20) and PN (GSC11 and GSC23) GSC lines were exposed to increasing concentrations and times of onalespib before being assayed for viability using the WST-1 assay in all four GSC lines *p<0.05. Data represents the mean ± SEM of triplicate values from two independent experiments. 

In vivo 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]


Kinase Assay:[2]
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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
Cell Research:[2]
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  • Cell lines: A375, 22RV1 and T474 cells
  • Concentrations: 1 μM
  • Incubation Time: 4 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Athymic BALB /c mice
  • Dosages: 80 mg/kg
  • Administration: Intraperitoneal adminis tration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 25 mg/mL (61.04 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O (prepare before use)
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 409.52


CAS No. 912999-49-6
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)C1=CC(=C(C=C1O)O)C(=O)N2CC3=C(C2)C=C(C=C3)CN4CCN(CC4)C

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    How to prepare the compound for in vivo studies?

  • Answer:

    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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID