Onalespib (lactate)

Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC) [1][2][3][4].

Product Specifications

CAS Number

[1019889-35-0]

Product Name Alternative

AT13387 (lactate)

UNSPSC

12352005

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/onalespib-lactate.html

Solubility

10 mM in DMSO

Smiles

C[C@H](O)C(O)=O.O=C(N1CC2=C(C=C(CN3CCN(C)CC3)C=C2)C1)C4=CC(C(C)C)=C(O)C=C4O

Molecular Formula

C27H37N3O6

Molecular Weight

499.60

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.