Onalespib

SKU: orb1300903

Description

Onalespib (AT13387) is an orally available small molecule Hsp90 inhibitor with antineoplastic potential. It disrupts Hsp90's chaperone function, leading to the degradation of client oncoproteins critical for tumor survival. This compound has demonstrated activity in preclinical studies across various cancer models, supporting its investigation in oncology research.

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 912999-49-6
• MW: 409.52
• Purity: 99.82% (May vary between batches)
• Formula: C₂₄H₃₁N₃O₃
• SMILES: CC(C)c1cc(C(=O)N2Cc3ccc(CN4CCN(C)CC4)cc3C2)c(O)cc1O
• Target: HSP
• Solubility: DMSO:2.04 mg/mL (4.98 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.44 mM)

Bioactivity

• Target IC50:
  HSP90 (AT13387):18 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.
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• 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.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AT 13387, AT13387, AT-13387, Onalespib, Onalespib (AT13387), inhibit, HSP, HSP90, Inhibitor, Heat shock proteins

Compound Identifiers

PubChem CID

11955716

Romy Cools # 1, Valeria Narykina # 1 2 3, Koen Vermeulen 4, Sanket J Mishra 5, Brian S J Blagg 5 6, Marleen Derweduwe 7 8 9, Frederik De Smet 7 8 9, Aaron Ziani-Zeryouh 10, Matteo Riva 10 11, An Coosemans 10, Frederic Rousseau 2 3, Joost Schymkowitz 2 3, Guy Bormans 12 [11C]HSP990 PET as a translational tool to investigate the role of Hsp90 in tumours and support the development of Hsp90 therapeutics EJNMMI Radiopharm Chem, (2025)

PubMed: 41003947