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.
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
Choose Selective HSP (e.g. HSP90) Inhibitors
|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.|
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. 
|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. |
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
|In vitro||DMSO||25 mg/mL (61.04 mM)|
|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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|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|
|NCT02097225||Recruiting||BRAF V600E Mutation Present|BRAF V600K Mutation Present|Metastatic Malignant Solid Neoplasm|Metastatic Melanoma|Stage III Cutaneous Melanoma AJCC v7|Stage IIIA Cutaneous Melanoma AJCC v7|Stage IIIB Cutaneous Melanoma AJCC v7|Stage IIIC Cutaneous Melanoma AJCC v7|Stage IV Cutaneous Melanoma AJCC v6 and v7|Unresectable Solid Neoplasm||National Cancer Institute (NCI)||May 29 2014||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|
|NCT02381535||Active not recruiting||Stage III Hypopharyngeal Squamous Cell Carcinoma AJCC v7|Stage III Laryngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage III Oral Cavity Squamous Cell Carcinoma AJCC v6 and v7|Stage III Oropharyngeal Squamous Cell Carcinoma AJCC v7|Stage IVA Hypopharyngeal Squamous Cell Carcinoma AJCC v7|Stage IVA Laryngeal Squamous Cell Carcinoma AJCC v7|Stage IVA Oral Cavity Squamous Cell Carcinoma AJCC v6 and v7|Stage IVA Oropharyngeal Squamous Cell Carcinoma AJCC v7|Stage IVB Hypopharyngeal Squamous Cell Carcinoma AJCC v7|Stage IVB Laryngeal Squamous Cell Carcinoma AJCC v7|Stage IVB Oral Cavity Squamous Cell Carcinoma AJCC v6 and v7|Stage IVB Oropharyngeal Squamous Cell Carcinoma AJCC v7||National Cancer Institute (NCI)||September 21 2015||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|
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
How to prepare the compound for in vivo studies?
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.