Onalespib

Onalespib (AT13387) is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor. Onalespib inhibits the proliferation, survival and migration. Onalespib decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib shows antitumor activity. Onalespib has the potential for the research of non-small cell lung cancer (NSCLC) [1][2][3].

Product Specifications

CAS Number

[912999-49-6]

Product Name Alternative

AT13387

UNSPSC

12352005

Hazard Statement

H302, H312, H332

Target

HSP

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/AT13387.html

Purity

99.92

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

OC1=CC(O)=C(C(C)C)C=C1C(N2CC(C=CC(CN3CCN(C)CC3)=C4)=C4C2)=O

Molecular Formula

C24H31N3O3

Molecular Weight

409.52

Precautions

H302, H312, H332

References & Citations

[1]Riess JW, et al. Erlotinib and Onalespib Lactate Focused on EGFR Exon 20 Insertion Non-Small Cell Lung Cancer (NSCLC) : A California Cancer Consortium Phase I/II Trial (NCI 9878) . Clin Lung Cancer. 2021 Nov;22 (6) :541-548. |[2]Canella A, et al. Efficacy of Onalespib, a Long-Acting Second-Generation HSP90 Inhibitor, as a Single Agent and in Combination with Temozolomide against Malignant Gliomas. Clin Cancer Res. 2017 Oct 15;23 (20) :6215-6226. |[3]Woodhead AJ, et al. Discovery of (2,4-dihydroxy-5-isopropylphenyl) -[5- (4-methylpiperazin-1-ylmethyl) -1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. J Med Chem. 2010 Aug 26;53 (16) :5956-69.|[4]Spiegelberg D, et al. The HSP90 inhibitor Onalespib exerts synergistic anti-cancer effects when combined with radiotherapy: an in vitro and in vivo approach. Sci Rep. 2020 Apr 3;10 (1) :5923.