Onalespib lactate  (Synonyms: AT13387 lactate)

Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an K_d 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].

Onalespib lactate (0-0.4 µM; 72 h, 48 h) inhibits the proliferation, survival and migration of glioma cells^[2].
Onalespib lactate (0-0.4 µM; 48 h) decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein in a dose-dependent manner^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Onalespib lactate (30 mg/kg; i.v.; once) crosses the blood-brain barrier (BBB) and causes sustained inhibition of HSP90 in 6-week-old ICR mice^[2].
Onalespib lactate (0.5 µM; from 5 to 10 days post-transplant) and TMZ (10 µM) reduce tumor growth and extend survival in zebrafish embryos^[2].
Onalespib lactate (5, 10 mg/kg for HCT116 xenografts, 20 mg/kg for A431 xenografts; i.p.; daily for 3 days) shows anti-tumor activity in HCT116 and A431 xenografts^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

499.60

C₂₇H₃₇N₃O₆

1019889-35-0

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [3]. 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.  [Content Brief]

  [4]. 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.  [Content Brief]