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Onalespib
🥰Excellent
Catalog No. T6284Cas No. 912999-49-6
Alias Onalespib (AT13387), AT13387
Onalespib (AT13387) is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Onalespib selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins.
Onalespib
🥰Excellent
Purity: 99.82%
Catalog No. T6284Alias Onalespib (AT13387), AT13387Cas No. 912999-49-6
Onalespib (AT13387) is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Onalespib selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $38 | In Stock | |
| 5 mg | $90 | In Stock | |
| 10 mg | $162 | In Stock | |
| 25 mg | $263 | In Stock | |
| 50 mg | $378 | In Stock | |
| 100 mg | $562 | In Stock | |
| 500 mg | $1,230 | In Stock |
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Purity:99.82%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Onalespib (AT13387) is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Onalespib selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins. |
| Targets&IC50 | HSP90 (AT13387):18 nM |
| In vitro | AT13387 is a potent inhibitor of the proliferation and survival of many different cell lines from a wide range of different tumor types (e.g., MES-SA cell line). In a panel of 30 tumor cell lines, AT13387 effectively inhibited cell proliferation with GI50 values in the range of 13-260 nM. AT13387 inhibited the proliferation of the non-tumorigenic human prostate epithelial cell line PNT2 with a GI50 value of 480 nM. |
| In vivo | AT13387 is a potent inhibitor of the proliferation and survival of many different cell lines from a wide range of different tumor types (e.g., MES-SA cell line). In a panel of 30 tumor cell lines, AT13387 effectively inhibited cell proliferation with GI50 values in the range of 13-260 nM. AT13387 inhibited the proliferation of the non-tumorigenic human prostate epithelial cell line PNT2 with a GI50 value of 480 nM. |
| Kinase Assay | 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 | 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) |
| Alias | Onalespib (AT13387), AT13387 |
| Molecular Weight | 409.52 |
| Formula | C24H31N3O3 |
| Cas No. | 912999-49-6 |
| Smiles | CC(C)c1cc(C(=O)N2Cc3ccc(CN4CCN(C)CC4)cc3C2)c(O)cc1O |
| Relative Density. | 1.237 g/cm3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||
| Solubility Information | DMSO: 2.04 mg/ml (5 mM）, Sonication is recommended.  | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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