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Onalespib

Catalog No. T6284   CAS 912999-49-6
Synonyms: AT13387, Onalespib (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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Onalespib Chemical Structure
Onalespib, CAS 912999-49-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
2 mg In stock $ 59.00
5 mg In stock $ 90.00
10 mg In stock $ 162.00
25 mg In stock $ 267.00
50 mg In stock $ 378.00
100 mg In stock $ 562.00
500 mg In stock $ 1,230.00
1 mL * 10 mM (in DMSO) In stock $ 90.00
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Purity: 99.82%
Purity: 98.05%
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Biological Description
Chemical Properties
Storage & Solubility Information
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
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)
Synonyms AT13387, Onalespib (AT13387)
Molecular Weight 409.52
Formula C24H31N3O3
CAS No. 912999-49-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.1 mg/mL (10 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Lyons J, et al.Poser A217. 2. Graham B, et al. Cancer Sci. 2012, 103(3), 522-527. 3. Wang Y, Ma H, Huang J, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors[J]. European Journal of Medicinal Chemistry. 2020: 113030.

TargetMolCitations

1. Wang Y, Ma H, Huang J, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. European Journal of Medicinal Chemistry,. 2021 Feb 15;212:113030

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Orally Active Compound Library Anti-Metabolism Disease Compound Library Anti-Lung Cancer Compound Library Exosome Compound Library Cytoskeletal Signaling Pathway Compound Library

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NDNA3 BX-2819 Pimitespib Triptolide VER-155008 NVP-HSP990 YUM70 Geldanamycin

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Onalespib 912999-49-6 Cytoskeletal Signaling Metabolism HSP AT13387 Heat shock proteins inhibit Inhibitor AT-13387 Onalespib (AT13387) AT 13387 inhibitor

 

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