Onalespib (AT13387)

Catalog No.S1163

Onalespib (AT13387) Chemical Structure

Molecular Weight(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.

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In DMSO USD 440 In stock
USD 270 In stock
USD 370 In stock
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2 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.

Purity & Quality Control

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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.
Targets
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 Mn31R5l1d3SxeHnjxsBie3OjeR?= NHPmPXJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgRYxidWG{IHLseYUh[XO|YYmsJGlEPTB;MD6wOFgh|ryP NEnVUngzODZ4MkWzOC=>
human HCT116 cells M4HiNXBzd2yrZnXyZZRqd25iYYPzZZk> M3jYelQ5KGh? Ml7LRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkC4JO69VQ>? MlPhNlQ4PjN{NkG=
human SKBR3 cells NUH1R2dMWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4qzWVQ5KGh? Mk\1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1LSN{Bk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMUSg{txO Mk\KNlQ4PjN{NkG=
human MCF7 cells MlrJVJJwdGmoZYLheIlwdiCjc4PhfS=> M164SVQ5KGh? MmHMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5{ODFOwG0> M{jUNVI1PzZ|Mk[x
human A231 cells NYLWSVZVWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4jl[|Q5KGh? NHW1[3JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyN|Eh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zLkCxJO69VQ>? NU\Ke4ZTOjR5NkOyOlE>
human HCT116 cells M1G4fWZ2dmO2aX;uJIF{e2G7 NH3xd24yOCCwTR?= MVuxPEBp M2LSdWlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBJe3B5MDDs[ZZmdCCjdDCxNEBvVSCjZoTldkAyQCCqcoOgZpkhcW2vdX7vZoxwfHSrbne= NH3lZpYzODZ4MkWzOC=>
human HCT116 cells M4X1UmZ2dmO2aX;uJIF{e2G7 M4e1XVMxKG6P MnnlNVghcA>? MljvTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFPET|QhdGW4ZXygZZQhOzBibl2gZYZ1\XJiMUigbJJ{KGK7IHntcZVvd2Kub4T0bY5o MV6yNFY3OjV|NB?=
human HCT116 cells NFrUWHFHfW6ldHnvckBie3OjeR?= MnTNN|Ahdk1? NE\GOW0yQCCq MnL1TY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIGLh[k0yKGyndnXsJIF1KDNyIH7NJIFnfGW{IEG4JIhzeyCkeTDpcY12dm:kbH;0eIlv\w>? M3;YRVIxPjZ{NUO0

... Click to View More Cell Line Experimental Data

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]

Protocol

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Athymic BALB /c mice
  • Formulation: 17.5% cyclodextrin
  • 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 individually and in order:
2% DMSO+30% PEG 300+ddH2O (prepare before use)
10mg/mL

* 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
Formula

C24H31N3O3

CAS No. 912999-49-6
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02898207 Not yet recruiting Estrogen Receptor Negative|HER2/Neu Negative|High Grade Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Metastatic 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 Solid Neoplasm National Cancer Institute (NCI) May 2017 Phase 1
NCT02503709 Recruiting Metastatic Solid Neoplasm|Unresectable Solid Neoplasm National Cancer Institute (NCI) April 2016 Phase 1
NCT02572453 Recruiting Anaplastic Large Cell Lymphoma, ALK-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 2016 Phase 2
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
NCT02535338 Recruiting Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer National Cancer Institute (NCI) January 2016 Phase 1|Phase 2
NCT02474173 Recruiting Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage III Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) January 2016 Phase 1

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