Onalespib (AT13387)

Catalog No.S1163

For research use only.

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.

Onalespib (AT13387) Chemical Structure

CAS No. 912999-49-6

Selleck's Onalespib (AT13387) has been cited by 19 publications

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 M1z4XWN6fG:2b4jpZ:Kh[XO|YYm= NX;3[JJ[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JGFt[W2jcjDicJVmKGG|c3H5MEBKSzVyPUCuNFQ5KM7:TR?= NXzQbmVkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2OlI2OzRpPkKwOlYzPTN2PD;hQi=>
human HCT116 cells MmjXSpVv[3Srb36gZZN{[Xl? M2GyPFExKG6P M{DJ[VE5KGh? MlHQTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJGh{eDdyIHzleoVtKGG2IEGwJI5OKGGodHXyJFE5KGi{czDifUBqdW23bn;icI91fGmwZx?= MoT2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4NkK1N|QoRjJyNk[yOVM1RC:jPh?=
human HCT116 cells MXTGeY5kfGmxbjDhd5NigQ>? NH;nfG4{OCCwTR?= NYnu[3dSOThiaB?= MmDqTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFPET|QhdGW4ZXygZZQhOzBibl2gZYZ1\XJiMUigbJJ{KGK7IHntcZVvd2Kub4T0bY5o MnPQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4NkK1N|QoRjJyNk[yOVM1RC:jPh?=
human HCT116 cells NWrUe3RvTnWwY4Tpc44h[XO|YYm= NXvjXJRqOzBibl2= NIrseVgyQCCq MoPSTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIGLh[k0yKGyndnXsJIF1KDNyIH7NJIFnfGW{IEG4JIhzeyCkeTDpcY12dm:kbH;0eIlv\w>? MlzoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4NkK1N|QoRjJyNk[yOVM1RC:jPh?=
human HCT116 cells MXLQdo9tcW[ncnH0bY9vKGG|c3H5 MV60PEBp MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMEig{txO NH7iNo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe2N|I3OSd-MkS3OlMzPjF:L3G+
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Assay
Methods Test Index PMID
Western blot AXL / c-Myc / p-Mnk1 / Mnk1 / p-eIF4E / eIF4E ; EGFR / p-EGFR / AKT / p-AKT / ERK / p-ERK / S6 / p-S6 ; HSP90 / HSP70 31431614 28679777
Growth inhibition assay Cell viability 28679777
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 (from reference)

Kinase Assay:[2]
  • 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]
  • 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]
  • 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.

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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)C1=CC(=C(C=C1O)O)C(=O)N2CC3=C(C2)C=C(C=C3)CN4CCN(CC4)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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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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